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Assay Detail

CHEMBL2212191

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

Binding
Inhibition of Hsp90alpha
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Heat shock protein HSP 90-alpha (CHEMBL3880)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

EC144 is a potent inhibitor of the heat shock protein 90.
Shi J, Van de Water R, Hong K, Lamer RB, Weichert KW, Sandoval CM, Kasibhatla SR, Boehm MF, Chao J, Lundgren K, Timple N, Lough R, Ibanez G, Boykin C, Burrows FJ, Kehry MR, Yun TJ, Harning EK, Ambrose C, Thompson J, Bixler SA, Dunah A, Snodgrass-Belt P, Arndt J, Enyedy IJ, Li P, Hong VS, McKenzie A, Biamonte MA.
J Med Chem (2012) 55 : 7786 -7795
PubMed 22938030 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 8.66 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2205798 1 9.15
CHEMBL2205245 1 9.00
CHEMBL1230584 1 8.96
CHEMBL2205799 1 8.70
CHEMBL560895 SNX-2112 -1.0 1 8.52
CHEMBL2205800 1 8.41
CHEMBL467399 BIIB021 2.0 1 8.29
CHEMBL2205244 1 8.22
CHEMBL252164 LUMINESPIB 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2205798 IC50 = 0.7 nM 9.15
CHEMBL2205245 IC50 = 1.0 nM 9.00
CHEMBL1230584 IC50 = 1.1 nM 8.96
CHEMBL2205799 IC50 = 2.0 nM 8.70
CHEMBL560895 SNX-2112 IC50 = 3.0 nM 8.52
CHEMBL2205800 IC50 = 3.9 nM 8.41
CHEMBL467399 BIIB021 IC50 = 5.1 nM 8.29
CHEMBL2205244 IC50 = 6.0 nM 8.22
CHEMBL252164 LUMINESPIB IC50 < 0.4 nM -