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Assay Detail

CHEMBL4182272

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

Binding
Inhibition of BRD2 in human HD-MB03 cells assessed as reduction in c-Myc protein expression after 72 hrs by Hoechst 33342 staining based immunofluorescence assay
2
Total Activities
1
Compounds Tested
2
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 2 (CHEMBL1293289)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Exploiting a water network to achieve enthalpy-driven, bromodomain-selective BET inhibitors.
Shadrick WR, Slavish PJ, Chai SC, Waddell B, Connelly M, Low JA, Tallant C, Young BM, Bharatham N, Knapp S, Boyd VA, Morfouace M, Roussel MF, Chen T, Lee RE, Kiplin Guy R, Shelat AA, Potter PM.
Bioorg Med Chem (2018) 26 : 25 -36
PubMed 29170024 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 6.32 6.32
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4209110 2 6.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4209110 EC50 = 480.0 nM 6.32
CHEMBL4209110 Inhibition - % -