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Assay Detail

CHEMBL4825231

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

Binding
Inhibition of ATAD2 (unknown origin) by TR-FRET assay
12
Total Activities
12
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

ATPase family AAA domain-containing protein 2 (CHEMBL2150837)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimization of Naphthyridones into Selective TATA-Binding Protein Associated Factor 1 (TAF1) Bromodomain Inhibitors.
Clegg MA, Theodoulou NH, Bamborough P, Chung CW, Craggs PD, Demont EH, Gordon LJ, Liwicki GM, Phillipou A, Tomkinson NCO, Prinjha RK, Humphreys PG.
ACS Med Chem Lett (2021) 12 : 1308 -1317
PubMed 34413961 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.50 6.20
pIC50 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4860188 1 6.20
CHEMBL4878541 1 6.00
CHEMBL4868866 1 5.90
CHEMBL3585461 1 5.80
CHEMBL3585452 1 5.70
CHEMBL4865495 1 5.70
CHEMBL4855456 1 5.60
CHEMBL4857270 1 5.00
CHEMBL4872504 1 5.00
CHEMBL4856376 1 4.90
CHEMBL4850335 1 4.70
CHEMBL4862754 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4860188 IC50 = 630.96 nM 6.20
CHEMBL4878541 IC50 = 1000.0 nM 6.00
CHEMBL4868866 IC50 = 1258.93 nM 5.90
CHEMBL3585461 IC50 = 1584.89 nM 5.80
CHEMBL3585452 IC50 = 1995.26 nM 5.70
CHEMBL4865495 IC50 = 1995.26 nM 5.70
CHEMBL4855456 IC50 = 2511.89 nM 5.60
CHEMBL4857270 IC50 = 10000.0 nM 5.00
CHEMBL4872504 IC50 = 10000.0 nM 5.00
CHEMBL4856376 IC50 = 12589.25 nM 4.90
CHEMBL4850335 IC50 = 19952.62 nM 4.70
CHEMBL4862754 pIC50 - -