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Assay Detail

CHEMBL3584050

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Modulation of P-gp (unknown origin) transfected in human MDA435/LCC6MDR cells assessed as reversible of paclitaxel resistance measured as IC50 for paclitaxel at 1 uM after 5 days by CellTiter 96 Aqueous assay
53
Total Activities
53
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

ATP-dependent translocase ABCB1 (CHEMBL4302)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potent and Nontoxic Chemosensitizer of P-Glycoprotein-Mediated Multidrug Resistance in Cancer: Synthesis and Evaluation of Methylated Epigallocatechin, Gallocatechin, and Dihydromyricetin Derivatives.
Wong IL, Wang BC, Yuan J, Duan LX, Liu Z, Liu T, Li XM, Hu X, Zhang XY, Jiang T, Wan SB, Chow LM.
J Med Chem (2015) 58 : 4529 -4549
PubMed 25985195 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 53 7.64 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3582168 1 8.57
CHEMBL3582155 1 8.52
CHEMBL3582156 1 8.48
CHEMBL3582149 1 8.43
CHEMBL3582170 1 8.38
CHEMBL3582167 1 8.34
CHEMBL3582154 1 8.21
CHEMBL3582169 1 8.18
CHEMBL3582153 1 8.09
CHEMBL3582148 1 8.06
CHEMBL3582180 1 8.03
CHEMBL3582166 1 7.94
CHEMBL3582165 1 7.93
CHEMBL3582162 1 7.92
CHEMBL3582139 1 7.92
CHEMBL3582159 1 7.87
CHEMBL3582158 1 7.87
CHEMBL3582182 1 7.84
CHEMBL3582143 1 7.83
CHEMBL3582157 1 7.80
CHEMBL3582179 1 7.80
CHEMBL3582152 1 7.75
CHEMBL3582164 1 7.73
CHEMBL3582151 1 7.72
CHEMBL3582137 1 7.71
CHEMBL1631996 1 7.68
CHEMBL3582147 1 7.66
CHEMBL3582146 1 7.60
CHEMBL3582178 1 7.58
CHEMBL3582183 1 7.56

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3582168 IC50 = 2.7 nM 8.57
CHEMBL3582155 IC50 = 3.0 nM 8.52
CHEMBL3582156 IC50 = 3.3 nM 8.48
CHEMBL3582149 IC50 = 3.7 nM 8.43
CHEMBL3582170 IC50 = 4.2 nM 8.38
CHEMBL3582167 IC50 = 4.6 nM 8.34
CHEMBL3582154 IC50 = 6.2 nM 8.21
CHEMBL3582169 IC50 = 6.6 nM 8.18
CHEMBL3582153 IC50 = 8.1 nM 8.09
CHEMBL3582148 IC50 = 8.7 nM 8.06
CHEMBL3582180 IC50 = 9.4 nM 8.03
CHEMBL3582166 IC50 = 11.6 nM 7.94
CHEMBL3582165 IC50 = 11.8 nM 7.93
CHEMBL3582139 IC50 = 12.0 nM 7.92
CHEMBL3582162 IC50 = 12.0 nM 7.92
CHEMBL3582159 IC50 = 13.4 nM 7.87
CHEMBL3582158 IC50 = 13.6 nM 7.87
CHEMBL3582182 IC50 = 14.4 nM 7.84
CHEMBL3582143 IC50 = 14.8 nM 7.83
CHEMBL3582157 IC50 = 15.7 nM 7.80
CHEMBL3582179 IC50 = 15.9 nM 7.80
CHEMBL3582152 IC50 = 18.0 nM 7.75
CHEMBL3582164 IC50 = 18.5 nM 7.73
CHEMBL3582151 IC50 = 19.0 nM 7.72
CHEMBL3582137 IC50 = 19.5 nM 7.71
CHEMBL1631996 IC50 = 21.0 nM 7.68
CHEMBL3582147 IC50 = 21.9 nM 7.66
CHEMBL3582146 IC50 = 25.0 nM 7.60
CHEMBL3582178 IC50 = 26.2 nM 7.58
CHEMBL3582183 IC50 = 27.8 nM 7.56
CHEMBL3582176 IC50 = 31.6 nM 7.50
CHEMBL3582145 IC50 = 32.2 nM 7.49
CHEMBL3582144 IC50 = 34.2 nM 7.47
CHEMBL3582142 IC50 = 36.0 nM 7.44
CHEMBL3582181 IC50 = 36.5 nM 7.44
CHEMBL3582174 IC50 = 36.6 nM 7.44
CHEMBL6966 VERAPAMIL IC50 = 38.0 nM 7.42
CHEMBL3582150 IC50 = 40.1 nM 7.40
CHEMBL3582177 IC50 = 40.7 nM 7.39
CHEMBL3582175 IC50 = 44.4 nM 7.35
CHEMBL3582136 IC50 = 45.2 nM 7.34
CHEMBL3582173 IC50 = 47.9 nM 7.32
CHEMBL3582163 IC50 = 49.0 nM 7.31
CHEMBL3582141 IC50 = 53.3 nM 7.27
CHEMBL3582161 IC50 = 67.1 nM 7.17
CHEMBL3582140 IC50 = 97.1 nM 7.01
CHEMBL3582172 IC50 = 107.3 nM 6.97
CHEMBL3582138 IC50 = 112.9 nM 6.95
CHEMBL297453 EPIGALOCATECHIN GALLATE IC50 = 124.1 nM 6.91
CHEMBL3582160 IC50 = 135.9 nM 6.87