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Assay Detail

CHEMBL3773446

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

Binding
Inhibition of BRD9 (unknown origin) incubated in dark for 30 mins by TR-FRET assay
14
Total Activities
14
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 9 (CHEMBL3108640)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition.
Theodoulou NH, Bamborough P, Bannister AJ, Becher I, Bit RA, Che KH, Chung CW, Dittmann A, Drewes G, Drewry DH, Gordon L, Grandi P, Leveridge M, Lindon M, Michon AM, Molnar J, Robson SC, Tomkinson NC, Kouzarides T, Prinjha RK, Humphreys PG.
J Med Chem (2016) 59 : 1425 -1439
PubMed 25856009 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 7.05 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3770188 1 8.10
CHEMBL3769944 1 8.00
CHEMBL3769688 1 7.90
CHEMBL3769855 1 7.90
CHEMBL3770949 1 7.80
CHEMBL3769509 1 7.40
CHEMBL3769628 1 7.40
CHEMBL3769507 1 7.30
CHEMBL3770367 1 7.10
CHEMBL3770039 1 6.90
CHEMBL3769979 1 6.70
CHEMBL3770716 1 5.50
CHEMBL3771218 1 5.40
CHEMBL3771308 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3770188 IC50 = 7.943 nM 8.10
CHEMBL3769944 IC50 = 10.0 nM 8.00
CHEMBL3769688 IC50 = 12.59 nM 7.90
CHEMBL3769855 IC50 = 12.59 nM 7.90
CHEMBL3770949 IC50 = 15.85 nM 7.80
CHEMBL3769509 IC50 = 39.81 nM 7.40
CHEMBL3769628 IC50 = 39.81 nM 7.40
CHEMBL3769507 IC50 = 50.12 nM 7.30
CHEMBL3770367 IC50 = 79.43 nM 7.10
CHEMBL3770039 IC50 = 125.89 nM 6.90
CHEMBL3769979 IC50 = 199.53 nM 6.70
CHEMBL3770716 IC50 = 3162.28 nM 5.50
CHEMBL3771218 IC50 = 3981.07 nM 5.40
CHEMBL3771308 IC50 = 5011.87 nM 5.30