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Assay Detail

CHEMBL5050325

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

Binding
Inhibition of BRD3-BD2 (unknown origin) assessed as dissociation constant by TR-FRET method
2
Total Activities
2
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 3 (CHEMBL1795186)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

CRCM5484: A BET-BDII Selective Compound with Differential Anti-leukemic Drug Modulation.
Carrasco K, Montersino C, Derviaux C, Saez-Ayala M, Hoffer L, Restouin A, Castellano R, Casassa J, Roche P, Pasquier E, Combes S, Morelli X, Collette Y, Betzi S.
J Med Chem (2022) 65 : 5660 -5674
PubMed 35348328 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.08 7.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4635134 GSK620 1 7.14
CHEMBL4636881 GSK046 1 7.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4635134 GSK620 IC50 = 72.0 nM 7.14
CHEMBL4636881 GSK046 IC50 = 98.0 nM 7.01