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Assay Detail

CHEMBL4030908

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

Binding
Inhibition of human BRPF2 (556 to 688 residues) expressed in Escherichia coli BL21 after 1 hr by BROMOscan assay
21
Total Activities
21
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

Bromodomain-containing protein 1 (CHEMBL2176774)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design of a Chemical Probe for the Bromodomain and Plant Homeodomain Finger-Containing (BRPF) Family of Proteins.
Igoe N, Bayle ED, Tallant C, Fedorov O, Meier JC, Savitsky P, Rogers C, Morias Y, Scholze S, Boyd H, Cunoosamy D, Andrews DM, Cheasty A, Brennan PE, Müller S, Knapp S, Fish PV.
J Med Chem (2017) 60 : 6998 -7011
PubMed 28714688 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 6.29 7.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3752151 1 7.34
CHEMBL4102050 1 7.32
CHEMBL4103077 1 7.10
CHEMBL4059962 1 7.00
CHEMBL4069814 1 6.89
CHEMBL4061727 1 6.82
CHEMBL4064071 1 6.82
CHEMBL4087315 1 6.72
CHEMBL4076056 1 6.70
CHEMBL4103432 1 6.57
CHEMBL4084805 1 6.42
CHEMBL4105505 1 6.29
CHEMBL4102751 1 6.28
CHEMBL4067436 1 5.85
CHEMBL4070377 1 5.77
CHEMBL4065116 1 5.48
CHEMBL4067917 1 5.36
CHEMBL4095325 1 5.17
CHEMBL4072276 1 5.11
CHEMBL4086558 1 4.85
CHEMBL4059509 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3752151 IC50 = 46.0 nM 7.34
CHEMBL4102050 IC50 = 48.0 nM 7.32
CHEMBL4103077 IC50 = 80.0 nM 7.10
CHEMBL4059962 IC50 = 100.0 nM 7.00
CHEMBL4069814 IC50 = 130.0 nM 6.89
CHEMBL4061727 IC50 = 150.0 nM 6.82
CHEMBL4064071 IC50 = 150.0 nM 6.82
CHEMBL4087315 IC50 = 190.0 nM 6.72
CHEMBL4076056 IC50 = 200.0 nM 6.70
CHEMBL4103432 IC50 = 270.0 nM 6.57
CHEMBL4084805 IC50 = 380.0 nM 6.42
CHEMBL4105505 IC50 = 510.0 nM 6.29
CHEMBL4102751 IC50 = 520.0 nM 6.28
CHEMBL4067436 IC50 = 1400.0 nM 5.85
CHEMBL4070377 IC50 = 1700.0 nM 5.77
CHEMBL4065116 IC50 = 3300.0 nM 5.48
CHEMBL4067917 IC50 = 4400.0 nM 5.36
CHEMBL4095325 IC50 = 6700.0 nM 5.17
CHEMBL4072276 IC50 = 7800.0 nM 5.11
CHEMBL4086558 IC50 = 14000.0 nM 4.85
CHEMBL4059509 IC50 > 100000.0 nM -