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Assay Detail

CHEMBL4614280

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

Binding
Inhibition of TRAP1 (unknown origin)
14
Total Activities
14
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

Heat shock protein 75 kDa, mitochondrial (CHEMBL1075132)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 2-((4-resorcinolyl)-5-aryl-1,2,3-triazol-1-yl)acetates as potent Hsp90 inhibitors with selectivity over TRAP1.
Jung S, Yoon NG, Yang S, Kim D, Lee WS, Hong KB, Lee C, Kang BH, Lee JH, Kang S.
Bioorg Med Chem Lett (2020) 30 : 126809 -126809
PubMed 31839539 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.07 7.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2103879 GANETESPIB 3.0 1 7.42
CHEMBL200102 PU-H71 2.0 1 6.48
CHEMBL4647894 1 5.16
CHEMBL4641526 1 5.07
CHEMBL4635982 1 4.92
CHEMBL4648091 1 4.85
CHEMBL4639163 1 4.80
CHEMBL4648197 1 4.80
CHEMBL4647171 1 4.76
CHEMBL4638275 1 4.61
CHEMBL4636983 1 4.61
CHEMBL4641450 1 4.59
CHEMBL4649532 1 4.48
CHEMBL4635778 1 4.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2103879 GANETESPIB IC50 = 37.7 nM 7.42
CHEMBL200102 PU-H71 IC50 = 330.6 nM 6.48
CHEMBL4647894 IC50 = 6983.0 nM 5.16
CHEMBL4641526 IC50 = 8480.0 nM 5.07
CHEMBL4635982 IC50 = 11883.0 nM 4.92
CHEMBL4648091 IC50 = 14147.0 nM 4.85
CHEMBL4639163 IC50 = 15974.0 nM 4.80
CHEMBL4648197 IC50 = 16014.0 nM 4.80
CHEMBL4647171 IC50 = 17362.0 nM 4.76
CHEMBL4638275 IC50 = 24515.0 nM 4.61
CHEMBL4636983 IC50 = 24487.0 nM 4.61
CHEMBL4641450 IC50 = 25448.0 nM 4.59
CHEMBL4649532 IC50 = 33173.0 nM 4.48
CHEMBL4635778 IC50 = 35102.0 nM 4.46