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Assay Detail

CHEMBL714116

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

Binding
Inhibitory activity against human transporter MRP1 (Multidrug resistance associated protein 1) expressed in COR.L23/R cell line
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Multidrug resistance-associated protein 1 (CHEMBL3004)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Studies on pyrrolopyrimidines as selective inhibitors of multidrug-resistance-associated protein in multidrug resistance.
Wang S, Folkes A, Chuckowree I, Cockcroft X, Sohal S, Miller W, Milton J, Wren SP, Vicker N, Depledge P, Scott J, Smith L, Jones H, Mistry P, Faint R, Thompson D, Cocks S.
J Med Chem (2004) 47 : 1329 -1338
PubMed 14998323 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 6.09 7.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27102 1 7.37
CHEMBL26485 1 7.21
CHEMBL280981 1 7.12
CHEMBL26635 1 6.98
CHEMBL286272 1 6.92
CHEMBL26599 1 6.86
CHEMBL282819 1 6.66
CHEMBL26795 1 6.64
CHEMBL282610 1 6.40
CHEMBL27172 1 6.39
CHEMBL27171 1 6.28
CHEMBL26892 1 6.27
CHEMBL283835 1 6.24
CHEMBL27861 1 6.22
CHEMBL27709 1 6.21
CHEMBL285576 1 6.19
CHEMBL282592 1 6.17
CHEMBL28098 1 6.16
CHEMBL27497 1 6.15
CHEMBL27823 1 6.05
CHEMBL28061 1 6.04
CHEMBL281252 1 6.04
CHEMBL27517 1 6.02
CHEMBL282151 1 5.86
CHEMBL26934 1 5.85
CHEMBL27834 1 5.73
CHEMBL26017 1 5.64
CHEMBL27452 1 5.55
CHEMBL281938 1 5.41
CHEMBL27841 1 5.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27102 IC50 = 43.0 nM 7.37
CHEMBL26485 IC50 = 61.0 nM 7.21
CHEMBL280981 IC50 = 76.0 nM 7.12
CHEMBL26635 IC50 = 105.0 nM 6.98
CHEMBL286272 IC50 = 120.0 nM 6.92
CHEMBL26599 IC50 = 138.0 nM 6.86
CHEMBL282819 IC50 = 218.0 nM 6.66
CHEMBL26795 IC50 = 229.0 nM 6.64
CHEMBL282610 IC50 = 399.0 nM 6.40
CHEMBL27172 IC50 = 410.0 nM 6.39
CHEMBL27171 IC50 = 523.0 nM 6.28
CHEMBL26892 IC50 = 533.0 nM 6.27
CHEMBL283835 IC50 = 570.0 nM 6.24
CHEMBL27861 IC50 = 600.0 nM 6.22
CHEMBL27709 IC50 = 620.0 nM 6.21
CHEMBL285576 IC50 = 650.0 nM 6.19
CHEMBL282592 IC50 = 675.0 nM 6.17
CHEMBL28098 IC50 = 690.0 nM 6.16
CHEMBL27497 IC50 = 715.0 nM 6.15
CHEMBL27823 IC50 = 887.0 nM 6.05
CHEMBL28061 IC50 = 920.0 nM 6.04
CHEMBL281252 IC50 = 910.0 nM 6.04
CHEMBL27517 IC50 = 955.0 nM 6.02
CHEMBL282151 IC50 = 1370.0 nM 5.86
CHEMBL26934 IC50 = 1415.0 nM 5.85
CHEMBL27834 IC50 = 1850.0 nM 5.73
CHEMBL26017 IC50 = 2300.0 nM 5.64
CHEMBL27452 IC50 = 2800.0 nM 5.55
CHEMBL281938 IC50 = 3900.0 nM 5.41
CHEMBL27841 IC50 = 6350.0 nM 5.20
CHEMBL282611 IC50 = 6300.0 nM 5.20
CHEMBL285830 IC50 = 6650.0 nM 5.18
CHEMBL26707 IC50 = 7350.0 nM 5.13
CHEMBL27634 IC50 = 9000.0 nM 5.05
CHEMBL27524 IC50 = 20900.0 nM 4.68
CHEMBL26530 IC50 > 50000.0 nM -