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Assay Detail

CHEMBL2212645

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

Binding
Inhibition of HSP90alpha in human MCF7 cells assessed as degradation of Her-2
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MCF7
Confidence 9 — Direct 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
EC50 11 7.60 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL252164 LUMINESPIB 2.0 1 8.15
CHEMBL2205799 1 8.05
CHEMBL109480 TANESPIMYCIN 3.0 1 7.92
CHEMBL1230584 1 7.85
CHEMBL2205798 1 7.82
CHEMBL560895 SNX-2112 -1.0 1 7.72
CHEMBL2205245 1 7.58
CHEMBL2205800 1 7.50
CHEMBL467399 BIIB021 2.0 1 7.42
CHEMBL2205243 1 7.01
CHEMBL2205244 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL252164 LUMINESPIB EC50 = 7.0 nM 8.15
CHEMBL2205799 EC50 = 9.0 nM 8.05
CHEMBL109480 TANESPIMYCIN EC50 = 12.0 nM 7.92
CHEMBL1230584 EC50 = 14.0 nM 7.85
CHEMBL2205798 EC50 = 15.0 nM 7.82
CHEMBL560895 SNX-2112 EC50 = 19.0 nM 7.72
CHEMBL2205245 EC50 = 26.0 nM 7.58
CHEMBL2205800 EC50 = 32.0 nM 7.50
CHEMBL467399 BIIB021 EC50 = 38.0 nM 7.42
CHEMBL2205243 EC50 = 98.0 nM 7.01
CHEMBL2205244 EC50 = 250.0 nM 6.60