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Assay Detail

CHEMBL1021614

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Binding
Binding affinity to HAT p300 catalytic domain by isothermal titration calorimetry
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

Mechanism of p300 specific histone acetyltransferase inhibition by small molecules.
Arif M, Pradhan SK, Thanuja GR, Vedamurthy BM, Agrawal S, Dasgupta D, Kundu TK.
J Med Chem (2009) 52 : 267 -277
PubMed 19086895 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 3 5.15 5.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL458934 CAMBOGIN 1 5.23
CHEMBL502489 GARCINOL 1 5.18
CHEMBL500215 1 5.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL458934 CAMBOGIN Kd = 5900.0 nM 5.23
CHEMBL502489 GARCINOL Kd = 6600.0 nM 5.18
CHEMBL500215 Kd = 9100.0 nM 5.04