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Assay Detail

CHEMBL4186385

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

Binding
Inhibition of recombinant His-tagged CBP (unknown origin) by TR-FRET assay
36
Total Activities
36
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

CREB-binding protein (CHEMBL5747)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of a biaryl series as inhibitors for the bromodomains of CBP/P300.
Lai KW, Romero FA, Tsui V, Beresini MH, de Leon Boenig G, Bronner SM, Chen K, Chen Z, Choo EF, Crawford TD, Cyr P, Kaufman S, Li Y, Liao J, Liu W, Ly J, Murray J, Shen W, Wai J, Wang F, Zhu C, Zhu X, Magnuson S.
Bioorg Med Chem Lett (2018) 28 : 15 -23
PubMed 29169673 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 7.42 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4217213 1 9.05
CHEMBL4208820 1 8.92
CHEMBL4203082 1 8.92
CHEMBL4204065 1 8.62
CHEMBL4207965 1 8.55
CHEMBL4204490 1 8.48
CHEMBL4209361 1 8.48
CHEMBL4215166 1 7.89
CHEMBL4209359 1 7.64
CHEMBL4214979 1 7.62
CHEMBL4217552 1 7.57
CHEMBL4218138 1 7.52
CHEMBL4207043 1 7.51
CHEMBL4209747 1 7.51
CHEMBL4213692 1 7.42
CHEMBL4208936 1 7.38
CHEMBL4207080 1 7.37
CHEMBL4203862 1 7.24
CHEMBL4214660 1 7.19
CHEMBL4210701 1 7.16
CHEMBL4215815 1 7.16
CHEMBL4218809 1 7.10
CHEMBL4204263 1 7.09
CHEMBL4210047 1 7.09
CHEMBL4214949 1 7.05
CHEMBL4203693 1 7.05
CHEMBL4210763 1 6.92
CHEMBL4206026 1 6.89
CHEMBL4215879 1 6.82
CHEMBL4207560 1 6.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4217213 IC50 = 0.9 nM 9.05
CHEMBL4208820 IC50 = 1.2 nM 8.92
CHEMBL4203082 IC50 = 1.2 nM 8.92
CHEMBL4204065 IC50 = 2.4 nM 8.62
CHEMBL4207965 IC50 = 2.8 nM 8.55
CHEMBL4204490 IC50 = 3.3 nM 8.48
CHEMBL4209361 IC50 = 3.3 nM 8.48
CHEMBL4215166 IC50 = 13.0 nM 7.89
CHEMBL4209359 IC50 = 23.0 nM 7.64
CHEMBL4214979 IC50 = 24.0 nM 7.62
CHEMBL4217552 IC50 = 27.0 nM 7.57
CHEMBL4218138 IC50 = 30.0 nM 7.52
CHEMBL4207043 IC50 = 31.0 nM 7.51
CHEMBL4209747 IC50 = 31.0 nM 7.51
CHEMBL4213692 IC50 = 38.0 nM 7.42
CHEMBL4208936 IC50 = 42.0 nM 7.38
CHEMBL4207080 IC50 = 43.0 nM 7.37
CHEMBL4203862 IC50 = 58.0 nM 7.24
CHEMBL4214660 IC50 = 65.0 nM 7.19
CHEMBL4215815 IC50 = 69.0 nM 7.16
CHEMBL4210701 IC50 = 69.0 nM 7.16
CHEMBL4218809 IC50 = 79.0 nM 7.10
CHEMBL4204263 IC50 = 81.0 nM 7.09
CHEMBL4210047 IC50 = 81.0 nM 7.09
CHEMBL4214949 IC50 = 90.0 nM 7.05
CHEMBL4203693 IC50 = 90.0 nM 7.05
CHEMBL4210763 IC50 = 120.0 nM 6.92
CHEMBL4206026 IC50 = 130.0 nM 6.89
CHEMBL4215879 IC50 = 150.0 nM 6.82
CHEMBL4207560 IC50 = 170.0 nM 6.77
CHEMBL4215949 IC50 = 180.0 nM 6.75
CHEMBL4202407 IC50 = 190.0 nM 6.72
CHEMBL4216533 IC50 = 240.0 nM 6.62
CHEMBL4210092 IC50 = 280.0 nM 6.55
CHEMBL4217633 IC50 = 650.0 nM 6.19
CHEMBL3959584 IC50 = 740.0 nM 6.13