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Assay Detail

CHEMBL5628522

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Binding
Inhibition of recombinant HDAC1 (unknown origin) using RHKK-Ac-AMC as substrate
17
Total Activities
17
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 deacetylase 1 (CHEMBL325)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of potent pyrrolo-pyrimidine and purine HDAC inhibitors for the treatment of advanced prostate cancer.
Moi D, Bonanni D, Belluti S, Linciano P, Citarella A, Franchini S, Sorbi C, Imbriano C, Pinzi L, Rastelli G.
Eur J Med Chem (2023) 260 : 115730 -115730
PubMed 37633202 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 5.43 8.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL99 TRICHOSTATIN 1.0 1 8.14
CHEMBL5629961 1 6.41
CHEMBL5631370 1 6.01
CHEMBL5633941 1 6.00
CHEMBL5631908 1 6.00
CHEMBL5632901 1 5.89
CHEMBL5633237 1 5.55
CHEMBL5631448 1 5.50
CHEMBL5632170 1 5.07
CHEMBL5632247 1 5.05
CHEMBL5631817 1 4.53
CHEMBL5631614 1 4.41
CHEMBL5633420 1 4.41
CHEMBL5632233 1 4.34
CHEMBL5633219 1 4.13
CHEMBL5632046 1 -
CHEMBL5631797 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL99 TRICHOSTATIN IC50 = 7.2 nM 8.14
CHEMBL5629961 IC50 = 390.0 nM 6.41
CHEMBL5631370 IC50 = 980.0 nM 6.01
CHEMBL5633941 IC50 = 1000.0 nM 6.00
CHEMBL5631908 IC50 = 990.0 nM 6.00
CHEMBL5632901 IC50 = 1300.0 nM 5.89
CHEMBL5633237 IC50 = 2800.0 nM 5.55
CHEMBL5631448 IC50 = 3200.0 nM 5.50
CHEMBL5632170 IC50 = 8560.0 nM 5.07
CHEMBL5632247 IC50 = 8900.0 nM 5.05
CHEMBL5631817 IC50 = 29300.0 nM 4.53
CHEMBL5631614 IC50 = 38800.0 nM 4.41
CHEMBL5633420 IC50 = 39000.0 nM 4.41
CHEMBL5632233 IC50 = 45400.0 nM 4.34
CHEMBL5633219 IC50 = 73300.0 nM 4.13
CHEMBL5632046 IC50 > 100000.0 nM -
CHEMBL5631797 IC50 > 100000.0 nM -