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Assay Detail

CHEMBL4182264

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

Functional
Cytotoxicity against human HD-MB03 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 5 6.43 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1957266 1 6.80
CHEMBL4209110 1 6.77
CHEMBL2177300 1 6.70
CHEMBL1232461 MOLIBRESIB 2.0 1 5.46
CHEMBL2393130 APABETALONE 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1957266 EC50 = 160.0 nM 6.80
CHEMBL4209110 EC50 = 170.0 nM 6.77
CHEMBL2177300 EC50 = 200.0 nM 6.70
CHEMBL1232461 MOLIBRESIB EC50 = 3500.0 nM 5.46
CHEMBL2393130 APABETALONE EC50 > 5000.0 nM -