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Assay Detail

CHEMBL4615391

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

Binding
Binding affinity to human partial length BRD9 (R130 to V259 residues) expressed in bacterial expression system by BROMOscan assay
18
Total Activities
18
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 9 (CHEMBL3108640)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Application of Atypical Acetyl-lysine Methyl Mimetics in the Development of Selective Inhibitors of the Bromodomain-Containing Protein 7 (BRD7)/Bromodomain-Containing Protein 9 (BRD9) Bromodomains.
Clegg MA, Bamborough P, Chung CW, Craggs PD, Gordon L, Grandi P, Leveridge M, Lindon M, Liwicki GM, Michon AM, Molnar J, Rioja I, Soden PE, Theodoulou NH, Werner T, Tomkinson NCO, Prinjha RK, Humphreys PG.
J Med Chem (2020) 63 : 5816 -5840
PubMed 32410449 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.06 8.70
IC50 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3769507 1 8.70
CHEMBL4642341 1 8.00
CHEMBL4648548 1 7.40
CHEMBL4645418 1 7.40
CHEMBL4639574 1 7.20
CHEMBL4643740 1 7.10
CHEMBL4635895 1 7.10
CHEMBL4642886 1 7.00
CHEMBL4644517 1 6.90
CHEMBL4634319 1 6.80
CHEMBL4645137 1 6.80
CHEMBL4642556 1 6.60
CHEMBL4636297 1 6.60
CHEMBL4646338 1 6.50
CHEMBL4632508 1 6.50
CHEMBL4635826 1 6.40
CHEMBL4641305 1 -
CHEMBL4635892 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3769507 Ki = 1.995 nM 8.70
CHEMBL4642341 Ki = 10.0 nM 8.00
CHEMBL4648548 Ki = 39.81 nM 7.40
CHEMBL4645418 Ki = 39.81 nM 7.40
CHEMBL4639574 Ki = 63.1 nM 7.20
CHEMBL4643740 Ki = 79.43 nM 7.10
CHEMBL4635895 Ki = 79.43 nM 7.10
CHEMBL4642886 Ki = 100.0 nM 7.00
CHEMBL4644517 Ki = 125.89 nM 6.90
CHEMBL4634319 Ki = 158.49 nM 6.80
CHEMBL4645137 Ki = 158.49 nM 6.80
CHEMBL4642556 Ki = 251.19 nM 6.60
CHEMBL4636297 Ki = 251.19 nM 6.60
CHEMBL4646338 Ki = 316.23 nM 6.50
CHEMBL4632508 Ki = 316.23 nM 6.50
CHEMBL4635826 Ki = 398.11 nM 6.40
CHEMBL4641305 IC50 > 50118.72 nM -
CHEMBL4635892 Ki > 10000.0 nM -