SW620 |
Cytotoxicity assay |
|
48 hrs |
Cytotoxicity against human SW620 cells assessed as cell viability after 48 hrs by MTT assay, IC50=25μM |
26197160 |
HepG2 |
Function assay |
10 uM |
90 mins |
Inhibition of P-gp mediated efflux in adriamycin-resistant human HepG2 cells assessed as intracellular rhodamine-123 accumulation at 10 uM incubated in dark condition for 90 mins by flow cytometry relative to control |
27328029 |
MDCK |
Function assay |
|
30 mins |
Activity at BCRP (unknown origin) expressed in MDCK cells using rhodamine 123 as substrate incubated for 30 mins prior to substrate addition measured after 30 mins by fluorometric analysis, EC50=0.01μM |
23374872 |
OVCAR8 |
Function assay |
1000 nM |
72 hrs |
Potentiation of cytotoxicity against human OVCAR8 cells assessed as IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 8.53 +/- 1.95 nM), IC50=0.00518μM |
27504669 |
K562/A02 |
Cytotoxicity assay |
|
48 hrs |
Cytotoxicity against human K562/A02 cells after 48 hrs by MTT assay, IC50=27.19μM |
28645831 |
Kb-V1 |
Function assay |
|
10 mins |
Inhibition of ABCB1 expressed in Kb-V1 cells after 10 mins by calcein-AM assay, IC50=0.223μM |
21570282 |
KBv1 |
Function assay |
|
|
Inhibition of ABCB1 overexpressed in human KBv1 cells by flow cytometric-based calcein-AM efflux assay, IC50=0.223μM |
19170519 |
KBV1 |
Function assay |
|
|
Inhibition of ABCB1 in human KBV1 cells assessed as inhibition of calcein-AM efflux, IC50=0.22μM |
26774038 |
A2780 |
Function assay |
|
30 mins |
Inhibition of human Pgp in A2780 cells after 30 mins by Hoechst 33342 assay, IC50=0.12589μM |
18083034 |
KB-3-1 |
Function assay |
1000 nM |
72 hrs |
Potentiation of doxorubicin-induced cytotoxicity against human KB-3-1 cells assessed as doxorubicin IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 0.15 +/- 0.04 uM), IC50=0.11μM |
27504669 |
OVCAR8 |
Function assay |
1000 nM |
72 hrs |
Potentiation of doxorubicin-induced cytotoxicity against human OVCAR8 cells assessed as doxorubicin IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 0.12 +/- 0.03 uM), IC50=0.08μM |
27504669 |
A2780/ADR |
Function assay |
|
|
Inhibition of P-glycoprotein-mediated multidrug resistance in adriamycin-resistant human A2780/ADR cells by calcein AM assay, IC50=0.078μM |
19250834 |
A2780adr |
Function assay |
|
|
Inhibition of P-gp expressed in A2780adr cells by calcein AM accumulation assay, IC50=0.08μM |
21354800 |
A2780 |
Function assay |
|
|
Inhibition of P-gp in human adriamycin-resistant A2780 cells by Hoechst 33342 assay, IC50=0.07244μM |
18678495 |
KBV1 |
Function assay |
1000 nM |
72 hrs |
Inhibition of human ABCB1 expressed in KBV1 cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring doxorubicin IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 5.07 +/- 0.19 uM), IC50=0.07μM |
27504669 |
CEM/VLB500 |
Function assay |
|
3 days |
Reversal of P-gp-mediated multidrug resistance to in human CEM/VLB500 cells after 3 days by resazurin assay, EC50=0.068μM |
17399990 |
EMT6/AR1.0 |
Function assay |
|
1 hr |
Inhibition of mouse Pgp in EMT6/AR1.0 cells after 1 hr by daunorubicin accumulation assay, IC50=0.06457μM |
18083034 |
EMT6/AR1.0 |
Function assay |
|
1 hr |
Inhibition of mouse Pgp in EMT6/AR1.0 cells after 1 hr by daunorubicin accumulation assay, IC50=0.064μM |
18083034 |
MDCK |
Function assay |
|
30 mins |
Inhibition of P-glycoprotein (unknown origin) expressed in MDCK cells assessed as reduction of calcein-AM transport after 30 mins by fluorescence assay, EC50=0.044μM |
24607999 |
MDCK |
Function assay |
|
30 mins |
Activity at MDR1 (unknown origin) expressed in MDCK cells using calcein AM as substrate incubated for 30 mins prior to substrate addition measured after 30 mins by fluorometric analysis, EC50=0.044μM |
23374872 |
NCI-ADR-RES |
Function assay |
1000 nM |
72 hrs |
Inhibition of human ABCB1 expressed in NCI-ADR-RES cells assessed as potentiation of cytotoxicity by measuring IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 3714.80 +/- 383.58 nM), IC50=0.01851μM |
27504669 |
KBV1 |
Function assay |
1000 nM |
72 hrs |
Inhibition of human ABCB1 expressed in KBV1 cells assessed as potentiation of cytotoxicity by measuring IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 277.68 +/- 56.61 nM), IC50=0.00066μM |
27504669 |
KBV1 |
Function assay |
|
10 mins |
Inhibition of ABCB1 in human KBV1 cells after 10 mins by Calcein-AM microplate assay, IC50=0.223μM |
24900683 |
MCF7/Topo |
Function assay |
|
|
Inhibition of ABCG2 overexpressed in human MCF7/Topo cells by flow cytometric-based mitoxantrone efflux assay, IC50=0.916μM |
19170519 |
MCF7/Topo |
Function assay |
|
2 hrs |
Inhibition of ABCG2 in human MCF7/Topo cells after 2 hrs by Hoechst 33342 staining based fluorescence assay, IC50=0.526μM |
30128080 |
MCF7/Topo |
Function assay |
|
2 hrs |
Inhibition of ABCG2 in human MCF7/Topo cells after 2 hrs by Hoechst 33342 microplate assay, IC50=0.526μM |
24900683 |
MCF7/Topo |
Function assay |
|
|
Inhibition of ABCG2 expressed in human MCF7/Topo cells by Hoechst microplate assay, IC50=0.526μM |
21570282 |
MCF7/Topo |
Function assay |
|
|
Inhibition of ABCG2 in human MCF7/Topo cells by Hoechst 33342 assay, IC50=0.52μM |
26774038 |
K562/A02 |
Function assay |
|
48 hrs |
Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring ADR IC50 measured after 48 hrs by MTT assay (Rvb = 51.34 +/- 5.1 uM), IC50=1.6μM |
28645831 |
MCF-7 MX |
Function assay |
|
|
Inhibition of BCRP expressed in MCF-7 MX cells using Hoechst 33342 staining, IC50=1.5μM |
21354800 |
MCF7 |
Function assay |
|
|
Inhibition of ABCG2 in human mitoxantrone-resistant MCF7 cells by Hoechst 33342 assay, IC50=1.44544μM |
18678495 |
HFE |
Cytotoxicity assay |
|
72 hrs |
Cytotoxicity against human HFE cells assessed as cell viability after 72 hrs by MTT assay, IC50=1.28μM |
26197160 |
MDCK |
Function assay |
|
|
Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining, IC50=0.94μM |
21354800 |
KBV |
Function assay |
5 uM |
72 hrs |
Reversal of P-gp-mediated drug resistance in human KBV cells assessed as potentiation of cytotoxicity by measuring IC50 at 5 uM after 72 hrs by MTT assay (Rvb = 398.34 +/- 0.58 uM), IC50=5.24μM |
30384042 |
K562/A02 |
Function assay |
|
48 hrs |
Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring ADR IC50 treated for 48 hrs followed by compound washout measured after 6 hrs by MTT assay (Rvb = 51.34 +/- 5.1 uM), IC50=4.97μM |
28645831 |
KBV |
Function assay |
10 uM |
72 hrs |
Reversal of P-gp-mediated drug resistance in human KBV cells assessed as potentiation of cytotoxicity by measuring IC50 at 10 uM after 72 hrs by MTT assay (Rvb = 398.34 +/- 0.58 uM), IC50=4.46μM |
30384042 |
K562/A02 |
Function assay |
|
48 hrs |
Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring ADR IC50 treated for 48 hrs followed by compound washout measured immediately by MTT assay (Rvb = 51.34 +/- 5.1 uM), IC50=3.02μM |
28645831 |
K562/A02 |
Function assay |
5 uM |
48 hrs |
Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring ADR IC50 at 5 uM measured after 48 hrs by MTT assay (Rvb = 43.75 to 96.91 uM), IC50=1.97μM |
28645831 |
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=0.03311μM |
22452412 |
MDCK |
Function assay |
|
|
Inhibition of MDR1 expressed in MDCK cells using rhodamine 123 staining by flow cytometry, IC50=0.21μM |
21354800 |
NCI-ADR-RES |
Function assay |
1000 nM |
72 hrs |
Inhibition of human ABCB1 expressed in NCI-ADR-RES cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring doxorubicin IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 5.54 +/- 0.60 uM), IC50=0.24μM |
27504669 |
MCF7 MX |
Function assay |
|
|
Inhibition of BCRP expressed in MCF7 MX cells by Hoechst 33342 staining, IC50=0.68μM |
19932960 |
MDCK |
Function assay |
|
|
Inhibition of BCRP expressed in MDCK cells by pheophorbide A assay, IC50=0.85μM |
19932960 |
K562/A02 |
Function assay |
|
48 hrs |
Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring ADR IC50 treated for 48 hrs followed by compound washout measured after 24 hrs by MTT assay (Rvb = 51.34 +/- 5.1 uM), IC50=14.39μM |
28645831 |
K562/A02 |
Function assay |
|
48 hrs |
Inhibition of ABCB1 in human K562/A02 cells assessed as potentiation of adriamycin-induced cytotoxicity by measuring ADR IC50 treated for 48 hrs followed by compound washout measured after 12 hrs by MTT assay (Rvb = 51.34 +/- 5.1 uM), IC50=8.28μM |
28645831 |
CCD-18Co |
Cytotoxicity assay |
|
48 hrs |
Cytotoxicity against human CCD-18Co cells assessed as cell viability after 48 hrs by MTT assay, IC50=25μM |
26197160 |
SW620/AD300 |
Cytotoxicity assay |
|
48 hrs |
Cytotoxicity against human SW620/AD300 cells assessed as cell viability after 48 hrs by MTT assay, IC50=25μM |
26197160 |
HLF |
Cytotoxicity assay |
|
48 hrs |
Cytotoxicity against HLF cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay, IC50=16.69μM |
27328029 |
CEM/VLB500 |
Growth inhibition assay |
|
3 days |
Growth inhibition of human CEM/VLB500 cells after 3 days by resazurin assay, GI50=13.5μM |
17399990 |
A2780adr |
Function assay |
10 uM |
30 mins |
Inhibition of ABCB1 in human A2780adr cells assessed as increase in accumulation of calcein AM at 10 uM preincubated for 30 mins followed by calcein AM addition measured every 60 secs for 60 mins by fluorescence assay relative to control |
29547272 |
K562/A02 |
Cytotoxicity assay |
|
48 hrs |
Cytotoxicity against human K562/A02 cells overexpressing P-gp assessed as reduction in cell viability after 48 hrs by MTT assay, IC50=27.19μM |
29631786 |
K562 |
Cytotoxicity assay |
|
48 hrs |
Cytotoxicity against human K562 cells after 48 hrs by MTT assay, IC50=31.56μM |
28645831 |
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 |
KB-V1 |
Function assay |
200 nM |
|
Inhibition of P-gp in human KB-V1 cells assessed as increase in rhodamine 123 accumulation at 200 nM |
21657271 |
NB1643 |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells |
29435139 |
SK-N-SH |
qHTS assay |
|
|
qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells |
29435139 |
HEK293 |
Function assay |
1000 nM |
72 hrs |
Potentiation of doxorubicin-induced cytotoxicity against HEK293 cells assessed as doxorubicin IC50 at 1000 nM after 72 hrs by CCK8 assay (Rvb = 5.28 +/- 0.74 nM), IC50=0.00495μM |
27504669 |
KB-3-1 |
Function assay |
1000 nM |
72 hrs |
Potentiation of cytotoxicity against human KB-3-1 cells assessed as IC50 at 1000 nM after 72 hrs by MTT assay (Rvb = 0.78 +/- 0.27 nM), IC50=0.00041μM |
27504669 |
HEK293 |
Function assay |
1000 nM |
72 hrs |
Inhibition of human ABCB1 transfected in HEK293 cells assessed as potentiation of doxorubicin-induced cytotoxicity by measuring doxorubicin IC50 at 1000 nM after 72 hrs by CCK8 assay (Rvb = 504.65 +/- 44.94 nM), IC50=0.02477μM |
27504669 |
HCT116 |
Cytotoxicity assay |
|
48 hrs |
Cytotoxicity against human HCT116 cells assessed as cell viability after 48 hrs by MTT assay, IC50=12.5μM |
26197160 |
MCF7/ADR |
Cytotoxicity assay |
|
48 hrs |
Intrinsic cytotoxicity against human MCF7/ADR cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay, IC50=13.1μM |
27328029 |
K562 |
Cytotoxicity assay |
|
48 hrs |
Cytotoxicity against human K562 cells assessed as reduction in cell viability after 48 hrs by MTT assay, IC50=31.56μM |
29631786 |
HepG2 |
Cytotoxicity assay |
|
48 hrs |
Cytotoxicity against adriamycin-resistant human HepG2 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay, IC50=37.2μM |
27328029 |
K562/DOX |
Function assay |
1 uM |
10 mins |
Inhibition of P-gp in human K562/DOX cells assessed as increase in rhodamine-123 efflux in human K562 cells at 1 uM incubated for 10 mins hrs by flow cytometry relative to untreated control |
28113128 |