human K562/R7 cells |
Function assay |
1 μM |
72 h |
Potentiation of doxorubicin-induced cytotoxicity against doxorubicin-resistant human K562/R7 cells assessed as doxorubicin IC50 at 1 uM after 72 hrs by MTT assay, IC50=0.7 μM |
25634041 |
MDCK2 |
Function assay |
10 uM |
40 mins |
Inhibition of human wild type Pgp expressed in MDCK2 cells assessed as calcein-AM accumulation at 10 uM after 40 mins. |
17964170 |
C2C12 |
Function assay |
0.1 ug/ml |
3 days |
Inhibition of hexose-6-phosphate dehydrogenase-induced cell differentiation in mouse C2C12 cells assessed as myosin heavy chain fluorescence at 0.1 ug/ml for 3 days. |
20081855 |
HCT116 |
Function assay |
10 uM |
30 mins |
Modulation of BCRP in human HCT116 cells assessed as intracellular accumulation of mitoxantrone at 10 uM after 30 mins by flow-cytometry. |
21488686 |
2008 |
Function assay |
10 uM |
30 mins |
Inhibition of human MRP1 expressed in 2008 cells at 10 uM preincubated for 30 mins prior to calcein AM addition measured every 60 secs up to 90 mins by calcein AM accumulation assay. |
23017888 |
A2780adr |
Function assay |
10 uM |
30 mins |
Inhibition of human P-gp overexpressed in doxorubicin resistant A2780adr cells at 10 uM preincubated for 30 mins prior to calcein AM addition measured every 60 secs up to 90 mins by calcein AM accumulation assay. |
23017888 |
HL60 |
Function assay |
5 uM |
40 mins |
Inhibition of Ca2+-induced mitochondrial permeability transition in human HL60 cells at 5 uM after 40 mins relative to control. |
23026083 |
Saos2 |
Function assay |
5 uM |
3 hrs |
Inhibition of p-gp in doxorubicin-resistant human Saos2 cells assessed as increase in doxorubicin uptake at 5 uM after 3 hrs by flow cytometric analysis. |
24720452 |
Saos2 |
Function assay |
5 uM |
2 hrs |
Inhibition of p-gp in doxorubicin-resistant human Saos2 cells assessed as increase in intracellular doxorubicin retention at 5 uM after 2 hrs by flow cytometric analysis. |
24720452 |
Saos2 |
Function assay |
5 uM |
2 to 3 hrs |
Inhibition of p-gp in doxorubicin-resistant human Saos2 cells assessed as intracellular doxorubicin distribution in nuclei at 5 uM after 2 to 3 hrs by laser scanning confocal microscopic analysis. |
24720452 |
A2780 |
Function assay |
5 uM |
40 mins |
Inhibition of Pgp-mediated drug efflux in adriamycin-resistant human A2780 cells assessed as increase in intracellular adriamycin level at 5 uM after 40 mins by flow cytometry analysis. |
24900323 |
A2780 |
Function assay |
5 uM |
1 hr |
Inhibition of Pgp-mediated drug efflux in adriamycin-resistant human A2780 cells assessed as increase in adriamycin uptake at 5 uM after 1 hr by flow cytometry analysis. |
24900323 |
A2780 |
Function assay |
5 uM |
8 hrs |
Inhibition of Pgp-mediated drug efflux in adriamycin-resistant human A2780 cells assessed as increase in adriamycin uptake at 5 uM after 8 hrs by flow cytometry analysis. |
24900323 |
T-cells |
Antiinflammatory assay |
0.01 to 100 nM |
2 days |
Antiinflammatory activity in LLO118 TCR transgenic mouse IL-2-competent CD4-positive T cells assessed as inhibition of LLO (190 to 205)-induced IL-2 production at 0.01 to 100 nM for 2 days by flow cytometric analysis. |
24900866 |
Th17 |
Antiinflammatory assay |
10 to 100 nM |
2 days |
Antiinflammatory activity in LLO118 TCR transgenic mouse Th17 cells assessed as inhibition of IL-17 production at 10 to 100 nM for 2 days by flow cytometric analysis. |
24900866 |
Th1 |
Antiinflammatory assay |
100 nM |
2 days |
Antiinflammatory activity in LLO118 TCR transgenic mouse Th1 cells assessed as inhibition of IFN-gamma production at 100 nM for 2 days by flow cytometric analysis. |
24900866 |
CD1 |
Function assay |
0.1 to 10 uM |
30 mins |
Inhibition of taurolithocholate acid 3-sulfate-induced necrosis in CD1 mouse pancreatic acinar cells at 0.1 to 10 uM after 30 mins by propidium iodide staining based confocal microscopic analysis. |
26950392 |
Flp-InTM-293 |
Function assay |
25 uM |
30 mins |
Inhibition of ABCC2 (unknown origin) expressed in human Flp-InTM-293 cells assessed as inhibition of calcein-AM efflux at 25 uM measured after 30 mins in presence of ABCB1 inhibitor GF120918 and ABCC1 inhibitor MK-571 by flow cytometry. |
27393949 |
hamster BHK21 |
Function assay |
25 uM |
30 mins |
Inhibition of human ABCC1 expressed in hamster BHK21 cells assessed as inhibition of calcein-AM efflux at 25 uM measured after 30 mins by flow cytometry. |
27393949 |
MDCK2 |
Function assay |
25 uM |
30 mins |
Inhibition of ABCC2 (unknown origin) expressed in MDCK2 cells assessed as inhibition of calcein-AM efflux at 25 uM measured after 30 mins in presence of ABCB1 inhibitor GF120918 and ABCC1 inhibitor MK-571 by flow cytometry. |
27393949 |
NH3T3 |
Function assay |
2.5 uM |
30 mins |
Inhibition of human ABCB1 expressed in mouse NH3T3 cells assessed as inhibition of calcein-AM efflux at 2.5 uM measured after 30 mins by flow cytometry. |
27393949 |
MDA435/LCC6MDR |
Function assay |
1 uM |
5 days |
Inhibition of P-gp in human MDA435/LCC6MDR cells assessed as potentiation of paclitaxel-induced cytotoxicity by measuring paclitaxel IC50 at 1 uM measured after 5 days by Cell Titer 96 Aqueous assay (Rvb = 139.3 +/- 7.5 nM), IC50 = 0.0018 μM. |
27750197 |
K562R |
Function assay |
5 uM |
1 hr |
Inhibition of P-gp in doxorubicin-resistant human K562R cells assessed as rhodamine efflux by measuring ratio of mean fluorescence intensity in presence and absence of compound at 5 uM incubated for 1 hr by flow cytometry. |
27753480 |
HCT15 |
Function assay |
0.4 to 6.3 ug/mL |
|
Modulation of P-gp in human HCT15 cells assessed as increase in DINIB-induced cytotoxicity at 0.4 to 6.3 ug/mL. |
11754602 |
UO31 |
Function assay |
0.4 to 6.3 ug/mL |
|
Modulation of P-gp in human UO31 cells assessed as increase in DINIB-induced cytotoxicity at 0.4 to 6.3 ug/mL. |
11754602 |
CAKI1 |
Function assay |
0.4 to 6.3 ug/mL |
|
Modulation of P-gp in human CAKI1 cells assessed as increase in DINIB-induced cytotoxicity at 0.4 to 6.3 ug/mL. |
11754602 |
HCT15 |
Function assay |
10 uM |
|
Inhibition of MDR1 in human HCT15 cells assessed as calcein-AM efflux at 10 uM by fluorescence assay. |
21348461 |
mouse L5178 cells |
Function assay |
|
20 mins |
Inhibition of human ABCB1-mediated rhodamine 123 efflux in mouse L5178 cells expressing human MDR1 after 20 mins by FACS analysis, IC50=0.65 μM |
21341745 |
KB/MDR cell |
Function assay |
|
72 h |
Inhibitory activity against KB/MDR cell line after 72 hr of drug exposure, IC50=1.5 μM |
15481991 |
human MDA435/LCC6MDR cells |
Cytotoxic assay |
|
72h |
Cytotoxicity against human MDA435/LCC6MDR cells expressing MDR after 72 hrs, IC50=2.8 μM |
22320402 |
human Huh5-2 cells |
Cytotoxic assay |
|
3 days |
Cytotoxicity against human Huh5-2 cells after 3 days by MTT assay , CC50=6 μM |
18625766 |
human HuH6 cells |
Cytotoxic assay |
|
3 days |
Cytotoxicity against human HuH6 cells after 3 days by MTT assay, CC50=7 μM |
18625766 |
human Huh-9-13 cells |
Cytotoxic assay |
|
3 days |
Cytotoxicity against human Huh-9-13 cells after 3 days by MTT assay, CC50=7 μM |
18625766 |
african green monkey Vero cells |
Function assay |
|
24 h |
Antiviral activity against West Nile virus infected in african green monkey Vero cells assessed as decrease in viral RNA synthesis after 24 hrs by luciferase reporter gene assay, IC50=8 μM |
19451286 |
human LCC-6 cells |
Cytotoxic assay |
|
72 h |
Cytotoxicity against human LCC-6 cells after 72 hrs, IC50=8.3 μM |
22320402 |
human Huh-Mono cells |
Cytotoxic assay |
|
3 days |
Cytotoxicity against human Huh-Mono cells after 3 days by MTT assay, CC50=24 μM |
18625766 |
mouse L929 cells |
Cytotoxic assay |
|
3 days |
Cytotoxicity against mouse L929 cells after 3 days by MTS assay, IC50=30 μM |
25985195 |
human MDA435/LCC6MDR cells |
Function assay |
|
5 days |
Modulation of P-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as reversing paclitaxel resistance measured as cell survival after 5 days by MTS assay, EC50=0.032 μM. |
25985195 |
mouse T cells |
Function assay |
|
4 days |
Immunosuppressive activity in mouse T cells assessed as inhibition of two way mixed lymphocyte reaction after 4 days by MTT assay, ic50=11 nM |
22984987 |
human splenocytes |
Function assay |
|
4 days |
Immunosuppressive activity in human splenocytes assessed as inhibition of [3H]thymidine incorporation after 4 days by allogenic mixed lymphocyte reaction assay, IC50=10 nM |
19827831 |
human Jurkat cells |
Function assay |
|
1 h |
Antiinflammatory activity in human Jurkat cells assessed as inhibition of anti-CD3/CD28 antibody-induced IL-2 production treated for 1 hr before anti-CD3/CD28 antibody challenge measured after 6 hrs by immunosuppression assay, EC50=5 nM |
19933795 |
human PBMC |
Function assay |
|
1 h |
Antiinflammatory activity in human PBMC assessed as inhibition of anti-CD3/CD28 antibody-induced IL-2 production treated for 1 hr before anti-CD3/CD28 antibody challenge measured after 6 hrs by immunosuppression assay, EC50=3.1 nM |
19933795 |
PMBC |
Function assay |
|
72 hrs |
Effect on proliferation of human peripheral blood mononuclear cells (PMBC) at 72 hr using MTT assay, IC50 = 8.97 μM. |
15203163 |
A2780 |
Function assay |
|
30 mins |
Inhibition of human Pgp in A2780 cells after 30 mins by Hoechst 33342 assay, IC50 = 1.41254 μM. |
18083034 |
A2780 |
Function assay |
|
30 mins |
Inhibition of human Pgp in A2780 cells after 30 mins by calcein AM assay, IC50 = 1.41254 μM. |
18083034 |
Huh-9-13 |
Antiviral assay |
|
3 days |
Antiviral activity against BILN 2061-resistant HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication after 3 days by quantitative RT-PCR, EC50 = 0.004 μM. |
19104013 |
Huh-9-13 |
Antiviral assay |
|
3 days |
Antiviral activity against compound-resistant HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication after 3 days by quantitative RT-PCR, EC50 = 0.35 μM. |
19104013 |
Huh-9-13 |
Antiviral assay |
|
3 days |
Antiviral activity against 2'-C-methyl-2'-fluoro-cytidine-resistant HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication after 3 days by quantitative RT-PCR, EC50 = 0.4 μM. |
19104013 |
Huh-9-13 |
Antiviral assay |
|
3 days |
Antiviral activity against VX 950-resistant HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication after 3 days by quantitative RT-PCR, EC50 = 0.49 μM. |
19104013 |
Huh-9-13 |
Antiviral assay |
|
3 days |
Antiviral activity against R479-resistant HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication after 3 days by quantitative RT-PCR, EC50 = 1.98 μM. |
19104013 |
Huh-9-13 |
Antiviral assay |
|
3 days |
Antiviral activity against cyclosporine-resistant HCV genotype 1b infected in human Huh-9-13 cells assessed as reduction in viral replication after 3 days by quantitative RT-PCR, EC50 = 3.85 μM. |
19104013 |
HuH7 |
Antiviral assay |
|
48 hrs |
Antiviral activity against HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay, EC50 = 0.21 μM. |
20176894 |
HuH7 |
Antiviral assay |
|
48 hrs |
Antiviral activity against cyclosporine A-resistant HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay, EC50 = 3.39 μM. |
20176894 |
T-cells |
Immunosuppressive assay |
|
72 hrs |
Immunosuppressive activity in BALB/c mouse T cells assessed as inhibition of anti-CD3/anti-CD28-stimulated cell proliferation after 72 hrs by MTT assay, IC50 = 0.06 μM. |
21131104 |
T-cells |
Cytotoxicity assay |
|
48 hrs |
Cytotoxicity against BALB/c mouse T cells after 48 hrs by MTT assay, CC50 = 15.82 μM. |
21131104 |
T-cells |
Immunosuppressive assay |
|
96 hrs |
Immunosuppressive activity in BALB/c/C57BL/6 mouse T cells assessed as inhibition of alloantigen-induced cell proliferation after 96 hrs by measuring [3H]thymidine uptake by mixed lymphocyte reaction assay, IC50 = 0.014 μM. |
21456524 |
L929 |
Cytotoxicity assay |
|
72 hrs |
Cytotoxicity against mouse L929 cells after 72 hrs, IC50 = 33.9 μM. |
22320402 |
CCRF-CEM/VCR1000 |
Function assay |
|
240 secs |
Inhibition of P-glycoprotein-mediated daunorubicin efflux from human CCRF-CEM/VCR1000 cells after 240 secs by FACS flow cytometric analysis, IC50 = 0.10233 μM. |
22452412 |
mouse lymph node cells |
Immunosuppressive assay |
|
72 hrs |
Immunosuppressive activity in anti-CD3/anti-CD8 co-stimulated Balb/c mouse lymph node cells assessed as inhibition of cell proliferation after 72 hrs by ELISA, IC50 = 0.07 μM. |
22494616 |
mouse lymph node cells |
Cytotoxicity assay |
|
48 hrs |
Cytotoxicity against Balb/c mouse lymph node cells after 48 hrs by MTT assay, CC50 = 10.1 μM. |
22494616 |
HEK293 |
Function assay |
|
5 mins |
Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting, Ki = 1.2 μM. |
22541068 |
HEK293 |
Function assay |
|
5 mins |
Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting, IC50 = 1.3 μM. |
22541068 |
HEK293 |
Function assay |
|
5 mins |
Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting, Ki = 36 μM. |
22541068 |
HEK293 |
Function assay |
|
5 mins |
Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting, IC50 = 37 μM. |
22541068 |
T-cells |
Immunosuppressive assay |
|
24 hrs |
Immunosuppressive activity in BALB/c mouse T cells assessed as inhibition of ConA-induced T cell proliferation incubated 24 hrs post ConA-induction for 72 hrs by MTT assay, IC50 = 2.12 μM. |
22727369 |
RPMI1788 |
Immunosuppressive assay |
|
6 days |
Immunosuppressive activity in human RPMI1788 cells cocultured with human PBMC assessed as inhibition of [3H]thymidine incorporation incubated for 6 days prior to [3H]thymidine addition measured after 18 hrs by liquid scintillation counting, IC50 = 0.054 μM. |
23347804 |
MT4 |
Antiviral assay |
|
4 days |
Antiviral activity against HIV1 3B infected in human MT4 cells coinfected with HTLV1 assessed as reduction in virus-induced cytopathogenicity after 4 days by MTT assay, EC50 = 0.45 μM. |
23849880 |
A2780Adr |
Function assay |
|
30 mins |
Inhibition of p-glycoprotein (unknown origin) expressed in human A2780Adr cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay, IC50 = 0.99 μM. |
23851114 |
2008 |
Function assay |
|
30 mins |
Inhibition of MRP1 (unknown origin) expressed in human 2008 cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay, IC50 = 2.81 μM. |
23851114 |
Jurkat T |
Function assay |
|
30 mins |
Inhibition of NFAT activation in PMA/ionomycin-stimulated human Jurkat T cells incubated for 30 mins prior to PMA/ionomycin stimulation measured after 5 hrs by luciferase reporter gene assay, IC50 = 0.0014 μM. |
23964991 |
MDA435/LCC6 |
Cytotoxicity assay |
|
3 days |
Cytotoxicity against human MDA435/LCC6 cells assessed as growth inhibition after 3 days by MTS assay, IC50 = 2.8 μM. |
24171478 |
MDA435/LCC6MDR |
Cytotoxicity assay |
|
3 days |
Cytotoxicity against human MDA435/LCC6MDR cells assessed as growth inhibition after 3 days by MTS assay, IC50 = 8.3 μM. |
24171478 |
L929 |
Cytotoxicity assay |
|
3 days |
Cytotoxicity against mouse L929 cells assessed as growth inhibition after 3 days by MTS assay, IC50 = 33.9 μM. |
24171478 |
A2780adr |
Function assay |
|
up to 90 mins |
Inhibition of MDR1 in human doxorubicin-resistant A2780adr cells assessed as Calcein AM accumulation treated 30 mins before Calcein AM addition measured up to 90 mins by fluorescence assay, IC50 = 0.92 μM. |
24184213 |
2008 |
Function assay |
|
up to 90 mins |
Inhibition of MRP1 in human 2008 cells assessed as Calcein AM accumulation treated 30 mins before Calcein AM addition measured up to 90 mins by fluorescence assay, IC50 = 2.7 μM. |
24184213 |
NCI/ADR-RES |
Function assay |
|
20 mins |
Inhibition of human P-glycoprotein expressed in NCI/ADR-RES cells assessed as reduction of calcein-AM transport after 20 mins by fluorescence assay. |
24992153 |
A2780adr |
Function assay |
|
90 mins |
Inhibition of ABCB1 in human A2780adr cells pre-incubated for 30 mins followed by calcein AM addition and further incubated for 60 mins by calcein AM assay, IC50 = 0.919 μM. |
25855895 |
T spleen cells |
Cytotoxicity assay |
|
72 hrs |
Cytotoxicity against ICR mouse T spleen cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 0.01 μM. |
26564266 |
B spleen cells |
Cytotoxicity assay |
|
72 hrs |
Cytotoxicity against ICR mouse B spleen cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 0.04 μM. |
26564266 |
RD |
Antiviral assay |
|
24 hrs |
Antiviral activity against EV71 infected in RD cells after 24 hrs by luciferase assay, EC50 = 3.66 μM. |
26564266 |
A2780/ADR |
Function assay |
|
30 mins |
Inhibition of ABCB1 in human A2780/ADR cells incubated for 30 mins measured up to 3600 secs with time intervals of 60 secs by calcein accumulation assay, IC50 = 1.41 μM. |
27100033 |
A2780/ADR |
Cytotoxicity assay |
|
72 hrs |
Cytotoxicity against human A2780/ADR cells overexpressing ABCB1 assessed as reduction in cell viability after 72 hrs by MTT assay, GI50 = 8.63 μM. |
27100033 |
A2780 |
Cytotoxicity assay |
|
72 hrs |
Cytotoxicity against human A2780 cells assessed as reduction in cell viability after 72 hrs by MTT assay, GI50 = 8.94 μM. |
27100033 |
Jurkat T |
Immunosuppressive assay |
|
13 hrs |
Immunosuppressive activity in human PMA/ionomycin stimulated Jurkat T cells assessed as suppression of IL2 production pretreated with cells followed by PMA/ionomycin stimulation measured after 13 hrs by ELISA, IC50 = 0.011 μM. |
27647370 |
A2780/ADR |
Function assay |
|
30 mins |
Inhibition of ABCB1 in human A2780/ADR cells assessed as reduction in calcien-AM efflux preincubated for 30 mins followed by calcien-AM addition measured immediately at 60 sec time interval for 60 mins by fluorescence assay, IC50 = 1.21 μM. |
27676469 |
HuH7 |
Antiviral assay |
|
72 hrs |
Antiviral activity against HCV genotype 1b Con1 infected in human HuH7 cells after 72 hrs by luciferase reporter gene assay, EC50 = 0.17 μM. |
28075591 |
HepaRG |
Antiviral assay |
|
16 hrs |
Antiviral activity against HBV infected in human HepaRG cells assessed as reduction in viral infection after 16 hrs, IC50 = 0.2 μM. |
28383274 |
replicon 2A cells |
Function assay |
|
72 hrs |
Inhibition of mTOR signaling pathway in (unknown origin) in sub-genomic replicon 2A cells assessed as reduction in phosphorylated rps6 protein levels up to 400 nM after 72 hrs by Western blot analysis. |
28442256 |
A2780adr |
Function assay |
|
30 mins |
Inhibition of ABCB1 in human A2780adr cells assessed as reduction in calcein AM levels preincubated for 30 mins followed by calcein AM addition measured immediately at 60 sec time interval for 60 mins by fluorescence assay, IC50 = 1.21 μM. |
28471656 |
H69AR |
Function assay |
|
30 mins |
Inhibition of ABCC1 in human H69AR cells assessed as reduction in calcein AM levels preincubated for 30 mins followed by calcein AM addition measured immediately at 60 sec time interval for 60 mins by fluorescence assay, IC50 = 2.97 μM. |
28471656 |
A2780/ADR |
Function assay |
|
30 mins |
Inhibition of ABCB1 in human A2780/ADR cells assessed as reduction in calcein-AM efflux preincubated for 30 mins followed by calcein-AM addition measured at 60 secs interval for 60 mins by fluorescence assay, IC50 = 1.21 μM. |
28841513 |
H69AR |
Function assay |
|
30 mins |
Inhibition of ABCC1 in human H69AR cells assessed as reduction in calcein-AM efflux preincubated for 30 mins followed by calcein-AM addition measured at 60 secs interval for 60 mins by fluorescence assay, IC50 = 3.53 μM. |
28841513 |
C57BL/6 mouse lymph node cells |
Immunosuppressive assay |
|
24 hrs |
Immunosuppressive activity in C57BL/6 mouse lymph node cells after 24 hrs by MTT assay, IC50 = 0.5 μM. |
29871844 |
HuH7 |
Antiviral assay |
|
3 days |
Antiviral activity against HCV genotype 2a infected in human HuH7 cells after 3 days by dual-glo luciferase reporter gene assay, EC50 = 0.773 μM. |
30074795 |
MT4 |
Cytotoxicity assay |
|
4 to 5 days |
Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 4 to 5 days by cell-titer glo assay, CC50 = 5.608 μM. |
30074795 |
mouse mammary carcinoma cell line EMT6/AR 1.0 |
Function assay |
|
|
Reversal effect on the accumulation of [3H]- daunorubicin in mouse mammary carcinoma cell line EMT6/AR 1.0, IC50=0.44 μM |
10098671 |
KB cell |
Function assay |
|
|
Inhibitory activity against KB cell line after 72 h of drug exposure, IC50=0.6 μM |
15481991 |
LLC-PK1 epithelial cells |
Function assay |
|
|
Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay, IC50=0.7 μM |
12699389 |
A2780/ADR cells |
Function assay |
|
|
Inhibition of P-glycoprotein expressed in A2780/ADR cells by calcein AM assay, IC50=1.41254 μM |
17890094 |
guinea pig ventricular myocytes |
Function assay |
|
|
Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes, IC50=2 μM |
22761000 |
human Caco2 cells |
Function assay |
|
|
nhibition of P-gp in human Caco2 cells assessed as reduction in digoxin efflux, IC50=2.9 μM |
23382458 |
leukemia CEM cells |
Function assay |
|
|
Inhibitory activity against Human MDR1 P-Glycoprotein ABC Transporter using leukemia CEM cells, IC50=3.4 μM |
12361387 |
human HeLa cells |
Function assay |
|
|
Antiviral activity against HPV-18 infected in human HeLa cells assessed as inhibition of viral replication after 7 days, TC50=4.6 μM |
18212100 |
human 2008 cells |
Function assay |
|
|
Inhibition of human MRP1 in human 2008 cells, IC50=4.78 μM |
18707884 |
human HuH7 cells |
Cytotoxic assay |
|
|
Cytotoxicity against human HuH7 cells assessed as release of lactate dehydrogenase, IC50=5.81 μM |
20943390 |
human HeLa cells |
Cytotoxic assay |
|
|
Cytotoxicity against human HeLa cells, TC50=8.3 μM |
18212100 |
MDCK cells |
Cytotoxic assay |
|
|
Cytotoxicity against MDCK cells, TC50=9.9 μM |
18212100 |
rat H42E cells |
Cytotoxic assay |
|
|
Cytotoxicity against rat H42E cells assessed as intracellular ATP level, TC50=42 μM |
19502058 |
CK1 cells |
Function assay |
|
|
Antiviral activity against HPV-33 infected in CK1 cells assessed as inhibition of viral replication after 7 days, TC50=0.3 μM |
18212100 |
HEK293 cells |
Function assay |
|
|
Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells assessed as protein-mediated pitavastatin uptake, Ki=0.2 μM |
22587986 |
human PBMC |
Proliferation assay |
|
|
Antiproliferative activity against human PBMC, IC50=12 nM |
15679309 |
human T-cell |
Function assay |
|
|
In vitro inhibitory activity against human T-cell production of lymphokine IL-2, IC50=8.1 nM |
7537331 |
Jurkat cells |
Function assay |
|
|
Immunosuppressive activity was measured by inhibition of the IL-2 production in Jurkat cells, IC50=2 nM |
14643337 |
HepG2 cells |
Function assay |
|
|
Inhibition of liver stage Plasmodium berghei infection in HepG2 cells, IC50=1.65 nM |
22586124 |
Jurkat |
Function assay |
|
|
The compound was tested in vitro for inhibition of IL-2 release stimulated with PMA/ionomycin by Jurkat cells., IC50 = 0.012 μM. |
7473543 |
mouse spleen cells |
Function assay |
|
|
The compound was tested in vitro for inhibition of proliferation in BDF1 mouse spleen cells stimulated with concanavalin A (ConA)., IC50 = 0.04 μM. |
7473543 |
Sf9 |
Function assay |
|
|
inhibition of Verapamil stimulated ATP hydrolysis in membranes from MDR1-expressing Sf9 cells, Ki = 0.02 μM. |
7514263 |
LLC-PK1 |
Function assay |
|
|
transepithelial transport (basal to apical) in MDR1-expressing LLC-PK1 cells, Km = 8.4 μM. |
7681059 |
HeLa |
Function assay |
|
|
inhibition of LTC4 uptake in membrane vesicle from MRP1-expressing HeLa cells, Ki = 5 μM. |
7961706 |
Caco-2 |
Function assay |
|
|
transepithelial transport (basal to apical) in Caco-2 cells, Km = 3.8 μM. |
8842452 |
spleen |
Function assay |
|
|
Effect of compound on IL-2 production from alloantigen-stimulated mouse spleen cells, IC50 = 0.01 μM. |
8893839 |
COS |
Function assay |
|
|
inhibition of Taurocholate uptake in ASBT-expressing COS cells, Ki = 24 μM. |
9458785 |
LLC-PK1 |
Function assay |
|
|
inhibition of Doxorubicin transepithelial transport (basal to apical) (Digoxin: 0.8 uM) in MDR1-expressing LLC-PK1 cells, IC50 = 3.66 μM. |
9914792 |
CEM/VLB100 |
Function assay |
|
|
inhibition of Calcein-AM efflux in CEM/VLB100 cells, Ki = 1.8 μM. |
10198227 |
HEK |
Function assay |
|
|
inhibition of BMG uptake in membrane vesicles from Mrp2-expressing HEK cells, Ki = 10 μM. |
10421658 |
HEK |
Function assay |
|
|
inhibition of BMG uptake in membrane vesicles from MRP2-expressing HEK cells, Ki = 21 μM. |
10421658 |
HeLa |
Function assay |
|
|
inhibition of Taurocholate uptake in NTCP-expressing HeLa cells, IC50 = 1 μM. |
10565843 |
LLC-PK1 |
Function assay |
|
|
inhibition of LTC4 uptake in membrane vesicles from MRP2-expressing LLC PK1 cells, Ki = 4.7 μM. |
10570049 |
Sf9 |
Function assay |
|
|
inhibition of Taurocholate uptake in membrane vesicles from Bsep-expressing Sf9 cells, Ki = 0.3 μM. |
10648470 |
Caco-2 |
Function assay |
|
|
inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells, IC50 = 1.3 μM. |
10820137 |
CEM/VLB100 |
Function assay |
|
|
inhibition of Calcein-AM efflux (Calcein-AM: 0.25 uM) in CEM/VLB100 cells, IC50 = 3.41 μM. |
10891114 |
Sf9 |
Function assay |
|
|
inhibition of ATPase in membrane vesicle from BCRP-expressing Sf9 cells, Ki = 0.5 μM. |
11437380 |
NIH-3T3-G185 |
Function assay |
|
|
inhibition of Daunorubicin efflux in NIH-3T3-G185 cells, IC50 = 1.4 μM. |
11716514 |
NIH-3T3-G185 |
Function assay |
|
|
inhibition of Calcein-AM efflux in NIH-3T3-G185 cells, IC50 = 1.7 μM. |
11716514 |
NIH-3T3-G185 |
Function assay |
|
|
inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells, IC50 = 1.7 μM. |
11716514 |
NIH-3T3-G185 |
Function assay |
|
|
inhibition of LDS-751 efflux in NIH-3T3-G185 cells, IC50 = 1.8 μM. |
11716514 |
NIH-3T3-G185 |
Function assay |
|
|
inhibition of Tetramethylrosamine efflux in NIH-3T3-G185 cells, IC50 = 2.1 μM. |
11716514 |
NIH-3T3-G185 |
Function assay |
|
|
inhibition of Fluo-3-AM efflux in NIH-3T3-G185 cells, IC50 = 2.4 μM. |
11716514 |
NIH-3T3-G185 |
Function assay |
|
|
inhibition of JC-1 efflux in NIH-3T3-G185 cells, IC50 = 4.3 μM. |
11716514 |
MDA-435/LCC6 and MDA-435/LCC6-MDRI |
Function assay |
|
|
Concentration that reduces the difference in reversal of DOX accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50%., EC50 = 0.5 μM. |
11784143 |
MDA-435/LCC6 |
Function assay |
|
|
Effect on reversal of [3H]- VBL accumulation in MDA-435/LCC6 (Pgp-negative) cells., EC50 = 0.6 μM. |
11784143 |
MDA-435/LCC6 and MDA-435/LCC6-MDRI |
Function assay |
|
|
Concentration that reduces difference in reversal of [3H]VBL accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50%, EC50 = 0.6 μM. |
11784143 |
MDA435/LCC6 MDR1 |
Function assay |
|
|
reversal of Vinblastine accumulation (Vinblastine: 0.005 uM) in MDA435/LCC6 MDR1 cells, EC50 = 0.6 μM. |
11784143 |
MDA-435/LCC6 (Pgp-negative) |
Function assay |
|
|
Effect on reversal of DOX accumulation in MDA-435/LCC6 (Pgp-negative) cells., EC50 = 0.7 μM. |
11784143 |
MDA-435/LCC6 |
Growth inhibitory assay |
|
|
Growth inhibitory activity on MDA-435/LCC6 (Pgp-positive) human breast cancer cells., IC50 = 1 μM. |
11784143 |
MDA-435/LCC6-MDRI |
Growth inhibitory assay |
|
|
Growth inhibitory activity on MDA-435/LCC6-MDRI (Pgp-negative) human breast cancer cells., IC50 = 1.1 μM. |
11784143 |
BTI-TN5B1-4 |
Function assay |
|
|
ATP hydrolysis in membrane fraction from High Five (BTI-TN5B1-4) cells, Km = 0.17 μM. |
11785684 |
Jurkat |
Function assay |
|
|
Inhibition of production of IL-2 secretion in Jurkat cells, IC50 = 0.007 μM. |
11881984 |
Jurkat |
Function assay |
|
|
Inhibition of production of beta-galactosidase IL-2 RGA in Jurkat cells, IC50 = 0.008 μM. |
11881984 |
LLC-PK1 |
Function assay |
|
|
increase in Vinblastine intracellular accumulation in MDR1-expressing LLC-PK1 cells, Ki = 1.3 μM. |
11961113 |
LLC-PK1 |
Function assay |
|
|
increase in Calcein-AM intracellular accumulation in MDR1-expressing LLC-PK1 cells, Ki = 4.66 μM. |
11961113 |
MDCK |
Function assay |
|
|
inhibition of Digoxin transepithelial transport (basal to apical) in MDR1-expressing MDCK cells, Ki = 2.18 μM. |
12134945 |
MDCK |
Function assay |
|
|
inhibition of Vinblastine transepithelial transport (basal to apical) in MRP2-expressing MDCK cells, Ki = 8.11 μM. |
12134946 |
LLC-PK1 |
Function assay |
|
|
increase in Calcein-AM intracellular accumulation in mdr1b-expressing LLC-PK1 cells, Ki = 3.5 μM. |
12235267 |
LLC-PK1 |
Function assay |
|
|
increase in Calcein-AM intracellular accumulation in mdr1a-expressing LLC-PK1 cells, Ki = 3.65 μM. |
12235267 |
HL-60 |
Function assay |
|
|
Inhibitory activity against Human formylpeptide receptor (FPR) of human leukemia HL-60 cells, IC20 = 3.6 μM. |
12361388 |
High Five cells |
Function assay |
|
|
inhibition of Taurochenodeoxycholate uptake(CsA 30uM, 30 % of control) in membrane vesicles prepared from High Five cells infected with the ABCB11 baculovirus, Ki = 9.5 μM. |
12404239 |
MDCKII |
Function assay |
|
|
inhibition of Cerivastatin uptake in OATP2-expressing MDCKII cells, Ki = 0.238 μM. |
12538813 |
Caco-2 |
Function assay |
|
|
transepithelial transport of digoxin (basal to apical) in Caco-2 cells, Ki = 0.35 μM. |
12636153 |
SK-E2 |
Function assay |
|
|
increase in bodipy intracellular accumulation (Bodipy: 0.2 uM) in SK-E2 cells (expressing BSEP), IC50 = 7.5 μM. |
12739759 |
SK-E2 |
Function assay |
|
|
increase in dihydrofluorescein intracellular accumulation (dihydrofluorescein: 1 uM) in SK-E2 cells (expressing BSEP), IC50 = 7.8 μM. |
12739759 |
HEK293 |
Function assay |
|
|
inhibition of Phalloidin uptake (Phalloidin: 1 uM) in OATP-C-expressing HEK293 cells, Ki = 0.2 μM. |
14530907 |
T-cells |
Function assay |
|
|
Inhibition of allogenic cells-stimulated proliferation in mouse T cells by mixed lymphocyte reaction method, IC50 = 0.032 μM. |
14593182 |
T-cells |
Function assay |
|
|
Inhibition of allogenic cells-stimulated proliferation in human T cells by mixed lymphocyte reaction method, IC50 = 0.074 μM. |
14593182 |
mouse spleen cells |
Cytotoxicity assay |
|
|
Cytotoxicity against BALB/c mouse spleen cells, CC50 = 1.35 μM. |
17081761 |
MDCK2 |
Function assay |
|
|
Inhibition of human MDR1-dependent accumulation of calcein-AM expressed in MDCK2 cells, IC50 = 9.34 μM. |
17664327 |
HEK293 |
Function assay |
|
|
Inhibition of cross-linking of human Pgp TM1 L65R/TM6 L339C/TM7 F728 mutant expressed in HEK293 cells assessed as drug level causing 50% inhibition of cross linking by immunoblot, Activity = 0.5 μM. |
17848563 |
HEK293 |
Function assay |
|
|
Inhibition of cross-linking of human Pgp TM6 L339C/TM7 F728C mutant expressed in HEK293 cells assessed as drug level causing 50% inhibition of cross linking by immunoblot, Activity = 0.6 μM. |
17848563 |
HEK293 |
Function assay |
|
|
Inhibition of cross-linking of human Pgp TM3T199R/TM6 L339C/TM7 F728C mutant expressed in HEK293 cells assessed as drug level causing 50% inhibition of cross linking by immunoblot, Activity = 1.1 μM. |
17848563 |
HEK293 |
Function assay |
|
|
Inhibition of cross-linking of human Pgp TM6 F343R/TM6 L339C/TM7 F728C mutant expressed in HEK293 cells assessed as drug level causing 50% inhibition of cross linking by immunoblot, Activity = 11 μM. |
17848563 |
HEK293 |
Function assay |
|
|
Inhibition of cross-linking of human Pgp TM5 I306R/TM6 L339C/TM7 F728C mutant expressed in HEK293 cells assessed as drug level causing 50% inhibition of cross linking by immunoblot, Activity = 15 μM. |
17848563 |
Caco-2 |
Function assay |
|
|
Inhibition of P-glycoprotein-mediated [3H]vinblastine transport in human Caco-2 cells, EC50 = 45.5 μM. |
18524592 |
A2780 |
Function assay |
|
|
Inhibition of P-gp in human adriamycin-resistant A2780 cells by Hoechst 33342 assay, IC50 = 1.41254 μM. |
18678495 |
A2780/ADR |
Function assay |
|
|
Inhibition of P-glycoprotein-mediated multidrug resistance in adriamycin-resistant human A2780/ADR cells by calcein AM assay, IC50 = 1.4 μM. |
19250834 |
C2C12 |
Function assay |
|
|
Inhibition of serum withdrawal-induced cell differentiation in mouse C2C12 cells assessed as myosin heavy chain expression. |
20081855 |
mouse spleen cells |
Function assay |
|
|
Inhibition of serine palmitoyltransferase in mouse spleen cells. |
21456524 |
Sf21 |
Function assay |
|
|
Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake, IC50 = 0.5 μM. |
21965623 |
Sf21 |
Function assay |
|
|
Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake, IC50 = 0.6 μM. |
21965623 |
T-cells |
Function assay |
|
|
Inhibition of CD4 expression in human CD4+ T cells, IC50 = 8.97 μM. |
22101135 |
HEK293 |
Function assay |
|
|
Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting, Ki = 1.3 μM. |
22541068 |
HEK293 |
Function assay |
|
|
Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting, IC50 = 1.4 μM. |
22541068 |
MDA435/LCC6MDR |
Function assay |
|
|
Modulation of p-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as reversal of paclitaxel resistance, EC50 = 0.032 μM. |
24171478 |
mouse |
Function assay |
|
|
Inhibition of human MDR1 expressed in mouse L5178 cells assessed as increase in intracellular accumulation of rhodamine 123 by FACSCalibur flow cytometry, IC50 = 0.67 μM. |
24900226 |
mouse lymph node cells |
Function assay |
|
|
Inhibition of PI3K-gamma in mouse lymph node cells assessed as inhibition of ConA-stimulated T cell proliferation, IC50 = 0.57 μM. |
26720154 |
MDCK2 |
Function assay |
|
|
Inhibition of ABCC2 (unknown origin) expressed in MDCK2 cells assessed as inhibition of calcein-AM efflux measured after 30 mins in presence of ABCB1 inhibitor GF120918 and ABCC1 inhibitor MK-571 by flow cytometry, IC50 = 25.6 μM. |
27393949 |
A673 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells. |
29435139 |
Saos-2 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells. |
29435139 |
BT-37 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells. |
29435139 |
RD |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells. |
29435139 |
MG 63 (6-TG R) |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells. |
29435139 |
NB1643 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells. |
29435139 |
OHS-50 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells. |
29435139 |
Rh41 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells. |
29435139 |
Rh30 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells. |
29435139 |
Rh41 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells. |
29435139 |
SK-N-MC |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells. |
29435139 |
Rh18 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells. |
29435139 |
SK-N-MC |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells. |
29435139 |
TC32 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells. |
29435139 |