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Assay Detail

CHEMBL4032869

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

Binding
Inhibition of His tagged recombinant CBP (unknown origin) by TR-FRET assay
26
Total Activities
26
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

A Unique Approach to Design Potent and Selective Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP) Inhibitors.
Bronner SM, Murray J, Romero FA, Lai KW, Tsui V, Cyr P, Beresini MH, de Leon Boenig G, Chen Z, Choo EF, Clark KR, Crawford TD, Jayaram H, Kaufman S, Li R, Li Y, Liao J, Liang X, Liu W, Ly J, Maher J, Wai J, Wang F, Zheng A, Zhu X, Magnuson S.
J Med Chem (2017) 60 : 10151 -10171
PubMed 29155580 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 6.86 8.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4061254 1 8.66
CHEMBL4068116 1 8.47
CHEMBL4095153 1 8.44
CHEMBL4073812 1 8.30
CHEMBL4065346 1 8.02
CHEMBL4076254 1 7.89
CHEMBL4072630 1 7.70
CHEMBL3814752 1 7.52
CHEMBL4059634 1 7.47
CHEMBL4095016 1 7.42
CHEMBL4097991 1 7.33
CHEMBL4064118 1 7.21
CHEMBL4081585 1 7.16
CHEMBL4068063 1 6.92
CHEMBL1621052 1 6.64
CHEMBL1738935 1 6.57
CHEMBL3774655 1 6.36
CHEMBL4086422 1 6.35
CHEMBL4077375 1 6.27
CHEMBL4070185 1 6.24
CHEMBL4068984 1 5.85
CHEMBL4097164 1 5.52
CHEMBL4094232 1 4.64
CHEMBL3448459 1 4.50
CHEMBL2270066 1 4.00
CHEMBL4072960 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4061254 IC50 = 2.2 nM 8.66
CHEMBL4068116 IC50 = 3.4 nM 8.47
CHEMBL4095153 IC50 = 3.6 nM 8.44
CHEMBL4073812 IC50 = 5.0 nM 8.30
CHEMBL4065346 IC50 = 9.5 nM 8.02
CHEMBL4076254 IC50 = 13.0 nM 7.89
CHEMBL4072630 IC50 = 20.0 nM 7.70
CHEMBL3814752 IC50 = 30.0 nM 7.52
CHEMBL4059634 IC50 = 34.0 nM 7.47
CHEMBL4095016 IC50 = 38.0 nM 7.42
CHEMBL4097991 IC50 = 47.0 nM 7.33
CHEMBL4064118 IC50 = 61.0 nM 7.21
CHEMBL4081585 IC50 = 69.0 nM 7.16
CHEMBL4068063 IC50 = 120.0 nM 6.92
CHEMBL1621052 IC50 = 230.0 nM 6.64
CHEMBL1738935 IC50 = 270.0 nM 6.57
CHEMBL3774655 IC50 = 440.0 nM 6.36
CHEMBL4086422 IC50 = 450.0 nM 6.35
CHEMBL4077375 IC50 = 540.0 nM 6.27
CHEMBL4070185 IC50 = 580.0 nM 6.24
CHEMBL4068984 IC50 = 1400.0 nM 5.85
CHEMBL4097164 IC50 = 3000.0 nM 5.52
CHEMBL4094232 IC50 = 23000.0 nM 4.64
CHEMBL3448459 IC50 = 32000.0 nM 4.50
CHEMBL2270066 IC50 = 99000.0 nM 4.00
CHEMBL4072960 IC50 > 100000.0 nM -