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Assay Detail

CHEMBL5376137

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

Binding
Inhibition of BRD4 BD2 (unknown origin) by TR-FRET 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 4 (CHEMBL1163125)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Guided Design of a Domain-Selective Bromodomain and Extra Terminal N-Terminal Bromodomain Chemical Probe.
Bradley E, Fusani L, Chung CW, Craggs PD, Demont EH, Humphreys PG, Mitchell DJ, Phillipou A, Rioja I, Shah RR, Wellaway CR, Prinjha RK, Palmer DS, Kerr WJ, Reid M, Wall ID, Cookson R.
J Med Chem (2023) 66 : 15728 -15749
PubMed 37967462 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 5.26 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4456922 1 6.40
CHEMBL5416784 1 6.30
CHEMBL5420656 1 6.30
CHEMBL5432176 1 6.20
CHEMBL5409942 1 5.90
CHEMBL5414030 1 5.60
CHEMBL5411322 1 5.40
CHEMBL5416283 1 5.30
CHEMBL5440431 1 5.10
CHEMBL5421774 1 5.10
CHEMBL5400900 1 5.00
CHEMBL5413795 1 5.00
CHEMBL5395952 1 4.90
CHEMBL5425663 1 4.90
CHEMBL5413916 1 4.80
CHEMBL5405343 1 4.80
CHEMBL5439597 1 4.70
CHEMBL5437203 1 4.70
CHEMBL5394124 1 4.70
CHEMBL5395658 1 4.70
CHEMBL5418662 1 4.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4456922 IC50 = 398.11 nM 6.40
CHEMBL5416784 IC50 = 501.19 nM 6.30
CHEMBL5420656 IC50 = 501.19 nM 6.30
CHEMBL5432176 IC50 = 630.96 nM 6.20
CHEMBL5409942 IC50 = 1258.93 nM 5.90
CHEMBL5414030 IC50 = 2511.89 nM 5.60
CHEMBL5411322 IC50 = 3981.07 nM 5.40
CHEMBL5416283 IC50 = 5011.87 nM 5.30
CHEMBL5440431 IC50 = 7943.28 nM 5.10
CHEMBL5421774 IC50 = 7943.28 nM 5.10
CHEMBL5400900 IC50 = 10000.0 nM 5.00
CHEMBL5413795 IC50 = 10000.0 nM 5.00
CHEMBL5395952 IC50 = 12589.25 nM 4.90
CHEMBL5425663 IC50 = 12589.25 nM 4.90
CHEMBL5413916 IC50 = 15848.93 nM 4.80
CHEMBL5405343 IC50 = 15848.93 nM 4.80
CHEMBL5439597 IC50 = 19952.62 nM 4.70
CHEMBL5437203 IC50 = 19952.62 nM 4.70
CHEMBL5394124 IC50 = 19952.62 nM 4.70
CHEMBL5395658 IC50 = 19952.62 nM 4.70
CHEMBL5418662 IC50 = 19952.62 nM 4.70