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Assay Detail

CHEMBL636772

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

Binding
Inhibition of ATP-ase activity in human colon tumor cell line (HCT116)
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Heat shock protein HSP90 (CHEMBL2095165)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Adenine derived inhibitors of the molecular chaperone HSP90-SAR explained through multiple X-ray structures.
Dymock B, Barril X, Beswick M, Collier A, Davies N, Drysdale M, Fink A, Fromont C, Hubbard RE, Massey A, Surgenor A, Wright L.
Bioorg Med Chem Lett (2004) 14 : 325 -328
PubMed 14698151 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 4.67 5.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL326082 1 5.39
CHEMBL109480 TANESPIMYCIN 3.0 1 4.87
CHEMBL326651 1 4.84
CHEMBL326564 1 4.82
CHEMBL109822 1 4.77
CHEMBL112953 1 4.52
CHEMBL113194 1 4.39
CHEMBL324951 1 4.27
CHEMBL109612 1 4.12
CHEMBL414883 RADICICOL 1 -
CHEMBL112896 1 -
CHEMBL113690 1 -
CHEMBL112834 1 -
CHEMBL326523 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL326082 IC50 = 4100.0 nM 5.39
CHEMBL109480 TANESPIMYCIN IC50 = 13400.0 nM 4.87
CHEMBL326651 IC50 = 14300.0 nM 4.84
CHEMBL326564 IC50 = 15300.0 nM 4.82
CHEMBL109822 IC50 = 17100.0 nM 4.77
CHEMBL112953 IC50 = 30000.0 nM 4.52
CHEMBL113194 IC50 = 41000.0 nM 4.39
CHEMBL324951 IC50 = 53500.0 nM 4.27
CHEMBL109612 IC50 = 75000.0 nM 4.12
CHEMBL414883 RADICICOL IC50 < 200.0 nM -
CHEMBL112896 IC50 > 200000.0 nM -
CHEMBL113690 IC50 > 200000.0 nM -
CHEMBL112834 IC50 > 200000.0 nM -
CHEMBL326523 IC50 > 200000.0 nM -