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Assay Detail

CHEMBL4189285

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

Binding
Displacement of (+)-JQ1 from 6H-Thr BRD4 Y97A mutant BD2 (unknown origin) after 30 mins by TR-FRET assay
ChEMBL ↗
51
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Bromodomain-containing protein 4 (CHEMBL1163125) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Tetrahydroquinoxalines as Bromodomain and Extra-Terminal Domain (BET) Inhibitors with Selectivity for the Second Bromodomain.
Law RP, Atkinson SJ, Bamborough P, Chung CW, Demont EH, Gordon LJ, Lindon M, Prinjha RK, Watson AJB, Hirst DJ.
J Med Chem (2018) 61 : 4317 -4334
PubMed 29656650 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 51 6.46 8.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2177300 — — 1 8.20
CHEMBL1957266 — — 1 7.30
CHEMBL4213809 — — 1 7.30
CHEMBL4205865 — — 1 7.30
CHEMBL4211868 — — 1 7.30
CHEMBL4218735 — — 1 7.20
CHEMBL4207924 — — 1 7.20
CHEMBL4205557 — — 1 7.20
CHEMBL4212836 — — 1 7.10
CHEMBL4213381 — — 1 7.00
CHEMBL4217789 — — 1 7.00
CHEMBL4208455 — — 1 7.00
CHEMBL4208993 — — 1 6.90
CHEMBL4216840 — — 1 6.90
CHEMBL4218207 — — 1 6.80
CHEMBL4206478 — — 1 6.80
CHEMBL4204112 — — 1 6.80
CHEMBL4204600 — — 3 6.70
CHEMBL4208636 — — 1 6.60
CHEMBL4210932 — — 1 6.50
CHEMBL4213572 — — 1 6.50
CHEMBL4204305 — — 1 6.40
CHEMBL4208576 — — 1 6.30
CHEMBL4206054 — — 1 6.30
CHEMBL4214299 — — 1 6.30
CHEMBL4214033 — — 1 6.30
CHEMBL4217264 — — 1 6.30
CHEMBL4216074 — — 1 6.20
CHEMBL4212964 — — 1 6.20
CHEMBL4202847 — — 1 6.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2177300 — IC50 = 6.31 nM 8.20
CHEMBL1957266 — IC50 = 50.12 nM 7.30
CHEMBL4211868 — IC50 = 50.12 nM 7.30
CHEMBL4205865 — IC50 = 50.12 nM 7.30
CHEMBL4213809 — IC50 = 50.12 nM 7.30
CHEMBL4218735 — IC50 = 63.1 nM 7.20
CHEMBL4207924 — IC50 = 63.1 nM 7.20
CHEMBL4205557 — IC50 = 63.1 nM 7.20
CHEMBL4212836 — IC50 = 79.43 nM 7.10
CHEMBL4217789 — IC50 = 100.0 nM 7.00
CHEMBL4208455 — IC50 = 100.0 nM 7.00
CHEMBL4213381 — IC50 = 100.0 nM 7.00
CHEMBL4208993 — IC50 = 125.89 nM 6.90
CHEMBL4216840 — IC50 = 125.89 nM 6.90
CHEMBL4204112 — IC50 = 158.49 nM 6.80
CHEMBL4206478 — IC50 = 158.49 nM 6.80
CHEMBL4218207 — IC50 = 158.49 nM 6.80
CHEMBL4204600 — IC50 = 199.53 nM 6.70
CHEMBL4208636 — IC50 = 251.19 nM 6.60
CHEMBL4210932 — IC50 = 316.23 nM 6.50
CHEMBL4213572 — IC50 = 316.23 nM 6.50
CHEMBL4204305 — IC50 = 398.11 nM 6.40
CHEMBL4204600 — IC50 = 501.19 nM 6.30
CHEMBL4206054 — IC50 = 501.19 nM 6.30
CHEMBL4208576 — IC50 = 501.19 nM 6.30
CHEMBL4214033 — IC50 = 501.19 nM 6.30
CHEMBL4217264 — IC50 = 501.19 nM 6.30
CHEMBL4214299 — IC50 = 501.19 nM 6.30
CHEMBL4216074 — IC50 = 630.96 nM 6.20
CHEMBL4212964 — IC50 = 630.96 nM 6.20
CHEMBL4203699 — IC50 = 630.96 nM 6.20
CHEMBL4202847 — IC50 = 630.96 nM 6.20
CHEMBL4203188 — IC50 = 794.33 nM 6.10
CHEMBL4216731 — IC50 = 794.33 nM 6.10
CHEMBL4206089 — IC50 = 794.33 nM 6.10
CHEMBL4215719 — IC50 = 794.33 nM 6.10
CHEMBL4210762 — IC50 = 794.33 nM 6.10
CHEMBL4213407 — IC50 = 1000.0 nM 6.00
CHEMBL4203288 — IC50 = 1000.0 nM 6.00
CHEMBL4211914 — IC50 = 1000.0 nM 6.00
CHEMBL4206502 — IC50 = 1258.93 nM 5.90
CHEMBL4206807 — IC50 = 1258.93 nM 5.90
CHEMBL4214313 — IC50 = 1258.93 nM 5.90
CHEMBL2393130 APABETALONE IC50 = 1584.89 nM 5.80
CHEMBL4206978 — IC50 = 1584.89 nM 5.80
CHEMBL4209650 — IC50 = 2511.89 nM 5.60
CHEMBL4210528 — IC50 = 2511.89 nM 5.60
CHEMBL4218053 — IC50 = 2511.89 nM 5.60
CHEMBL4210130 — IC50 = 5011.87 nM 5.30
CHEMBL4204600 — IC50 > 50118.72 nM -