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Assay Detail

CHEMBL4185404

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

Functional
Growth inhibition of human MV4-11 cells after 4 days by WST-8 assay
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MV4-11
Confidence 1 — Organism
Curated By Intermediate

Target

MV4-11 (CHEMBL613835)
Type CELL-LINE
Organism Homo sapiens

Publication

Structure-Based Discovery of 4-(6-Methoxy-2-methyl-4-(quinolin-4-yl)-9H-pyrimido[4,5-b]indol-7-yl)-3,5-dimethylisoxazole (CD161) as a Potent and Orally Bioavailable BET Bromodomain Inhibitor.
Zhao Y, Bai L, Liu L, McEachern D, Stuckey JA, Meagher JL, Yang CY, Ran X, Zhou B, Hu Y, Li X, Wen B, Zhao T, Li S, Sun D, Wang S.
J Med Chem (2017) 60 : 3887 -3901
PubMed 28463487 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 7.24 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4164015 1 8.70
CHEMBL4214978 1 8.29
CHEMBL4215403 1 8.22
CHEMBL4208405 1 8.18
CHEMBL4210062 1 7.89
CHEMBL4211972 1 7.89
CHEMBL4212515 1 7.82
CHEMBL4203276 1 7.77
CHEMBL3581661 1 7.70
CHEMBL1957266 1 7.62
CHEMBL4171228 1 7.58
CHEMBL4208561 1 7.55
CHEMBL4207609 1 7.54
CHEMBL4210754 1 7.33
CHEMBL4209113 1 7.24
CHEMBL4218757 1 7.16
CHEMBL4211497 1 7.12
CHEMBL4207024 1 7.11
CHEMBL1232461 MOLIBRESIB 2.0 1 7.03
CHEMBL4203725 1 7.02
CHEMBL4210981 1 7.00
CHEMBL4213494 1 7.00
CHEMBL2017291 1 6.79
CHEMBL4215941 1 6.74
CHEMBL4218866 1 6.72
CHEMBL4207729 1 6.60
CHEMBL4209937 1 6.53
CHEMBL4205577 1 6.48
CHEMBL4202675 1 6.37
CHEMBL4212636 1 5.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4164015 IC50 = 2.0 nM 8.70
CHEMBL4214978 IC50 = 5.1 nM 8.29
CHEMBL4215403 IC50 = 6.0 nM 8.22
CHEMBL4208405 IC50 = 6.6 nM 8.18
CHEMBL4210062 IC50 = 13.0 nM 7.89
CHEMBL4211972 IC50 = 13.0 nM 7.89
CHEMBL4212515 IC50 = 15.0 nM 7.82
CHEMBL4203276 IC50 = 17.0 nM 7.77
CHEMBL3581661 IC50 = 20.0 nM 7.70
CHEMBL1957266 IC50 = 24.0 nM 7.62
CHEMBL4171228 IC50 = 26.0 nM 7.58
CHEMBL4208561 IC50 = 28.0 nM 7.55
CHEMBL4207609 IC50 = 29.0 nM 7.54
CHEMBL4210754 IC50 = 47.0 nM 7.33
CHEMBL4209113 IC50 = 57.0 nM 7.24
CHEMBL4218757 IC50 = 69.0 nM 7.16
CHEMBL4211497 IC50 = 76.0 nM 7.12
CHEMBL4207024 IC50 = 77.0 nM 7.11
CHEMBL1232461 MOLIBRESIB IC50 = 93.0 nM 7.03
CHEMBL4203725 IC50 = 95.0 nM 7.02
CHEMBL4210981 IC50 = 99.0 nM 7.00
CHEMBL4213494 IC50 = 99.0 nM 7.00
CHEMBL2017291 IC50 = 162.0 nM 6.79
CHEMBL4215941 IC50 = 182.0 nM 6.74
CHEMBL4218866 IC50 = 190.0 nM 6.72
CHEMBL4207729 IC50 = 253.0 nM 6.60
CHEMBL4209937 IC50 = 295.0 nM 6.53
CHEMBL4205577 IC50 = 334.0 nM 6.48
CHEMBL4202675 IC50 = 423.0 nM 6.37
CHEMBL4212636 IC50 = 1062.0 nM 5.97
CHEMBL4217058 IC50 = 2863.0 nM 5.54
CHEMBL4216942 IC50 > 10000.0 nM -
CHEMBL4215450 IC50 > 10000.0 nM -
CHEMBL4210448 IC50 > 1000.0 nM -