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Assay Detail

CHEMBL5033899

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

Binding
Inhibition of p300 (unknown origin) preincubated for 15 mins followed by addition of substrate [3H] Ac-CoA and measured after 60 mins by liquid scintillation counting assay
16
Total Activities
16
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

Histone acetyltransferase p300 (CHEMBL3784)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis and biological evaluation of a novel spiro oxazolidinedione as potent p300/CBP HAT inhibitor for the treatment of ovarian cancer.
Ding H, Pei Y, Li Y, Xu W, Mei L, Hou Z, Guang Y, Cao L, Li P, Cao H, Bian J, Chen K, Luo C, Zhou B, Zhang T, Li Z, Yang Y.
Bioorg Med Chem (2021) 52 : 116512 -116512
PubMed 34801827 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 8.26 9.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5090239 1 9.31
CHEMBL5082755 1 9.25
CHEMBL4475351 1 9.02
CHEMBL5083020 1 8.77
CHEMBL5077158 1 8.66
CHEMBL4524352 1 8.60
CHEMBL5094423 1 8.40
CHEMBL5081689 1 8.07
CHEMBL5078353 1 8.07
CHEMBL5078021 1 8.01
CHEMBL5085891 1 8.00
CHEMBL5083262 1 7.96
CHEMBL5073432 1 7.92
CHEMBL5084035 1 7.89
CHEMBL4282264 A-485 1 7.82
CHEMBL5089370 1 6.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5090239 IC50 = 0.49 nM 9.31
CHEMBL5082755 IC50 = 0.56 nM 9.25
CHEMBL4475351 IC50 = 0.95 nM 9.02
CHEMBL5083020 IC50 = 1.7 nM 8.77
CHEMBL5077158 IC50 = 2.2 nM 8.66
CHEMBL4524352 IC50 = 2.5 nM 8.60
CHEMBL5094423 IC50 = 4.0 nM 8.40
CHEMBL5081689 IC50 = 8.6 nM 8.07
CHEMBL5078353 IC50 = 8.6 nM 8.07
CHEMBL5078021 IC50 = 9.8 nM 8.01
CHEMBL5085891 IC50 = 10.0 nM 8.00
CHEMBL5083262 IC50 = 11.0 nM 7.96
CHEMBL5073432 IC50 = 12.0 nM 7.92
CHEMBL5084035 IC50 = 13.0 nM 7.89
CHEMBL4282264 A-485 IC50 = 15.0 nM 7.82
CHEMBL5089370 IC50 = 430.0 nM 6.37