Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1026068

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

Binding
Inhibition of Hsp90 in human AU565 cells assessed as Her2 degradation after 24 hrs by high content screening
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type AU565
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Discovery of novel 2-aminobenzamide inhibitors of heat shock protein 90 as potent, selective and orally active antitumor agents.
Huang KH, Veal JM, Fadden RP, Rice JW, Eaves J, Strachan JP, Barabasz AF, Foley BE, Barta TE, Ma W, Silinski MA, Hu M, Partridge JM, Scott A, DuBois LG, Freed T, Steed PM, Ommen AJ, Smith ED, Hughes PF, Woodward AR, Hanson GJ, McCall WS, Markworth CJ, Hinkley L, Jenks M, Geng L, Lewis M, Otto J, Pronk B, Verleysen K, Hall SE.
J Med Chem (2009) 52 : 4288 -4305
PubMed 19552433 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 37 5.40 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL109480 TANESPIMYCIN 3.0 1 8.52
CHEMBL560955 1 7.34
CHEMBL562990 1 6.31
CHEMBL559840 1 5.80
CHEMBL552300 1 5.79
CHEMBL563335 1 5.74
CHEMBL553939 1 5.30
CHEMBL554288 1 5.19
CHEMBL563608 1 5.16
CHEMBL563500 1 5.05
CHEMBL560895 SNX-2112 -1.0 1 5.00
CHEMBL561019 1 4.80
CHEMBL564211 1 4.52
CHEMBL561497 1 4.46
CHEMBL558876 1 4.34
CHEMBL538683 1 4.30
CHEMBL549744 1 4.19
CHEMBL551293 1 -
CHEMBL564702 1 -
CHEMBL552094 1 -
CHEMBL556878 1 -
CHEMBL561224 1 -
CHEMBL549543 1 -
CHEMBL562038 1 -
CHEMBL562037 1 -
CHEMBL551699 1 -
CHEMBL561498 1 -
CHEMBL550139 1 -
CHEMBL561637 1 -
CHEMBL564559 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL109480 TANESPIMYCIN IC50 = 3.0 nM 8.52
CHEMBL560955 IC50 = 46.0 nM 7.34
CHEMBL562990 IC50 = 490.0 nM 6.31
CHEMBL559840 IC50 = 1590.0 nM 5.80
CHEMBL552300 IC50 = 1610.0 nM 5.79
CHEMBL563335 IC50 = 1830.0 nM 5.74
CHEMBL553939 IC50 = 5000.0 nM 5.30
CHEMBL554288 IC50 = 6400.0 nM 5.19
CHEMBL563608 IC50 = 7000.0 nM 5.16
CHEMBL563500 IC50 = 9000.0 nM 5.05
CHEMBL560895 SNX-2112 IC50 = 10000.0 nM 5.00
CHEMBL561019 IC50 = 16000.0 nM 4.80
CHEMBL564211 IC50 = 30000.0 nM 4.52
CHEMBL561497 IC50 = 35000.0 nM 4.46
CHEMBL558876 IC50 = 46000.0 nM 4.34
CHEMBL538683 IC50 = 50000.0 nM 4.30
CHEMBL549744 IC50 = 64000.0 nM 4.19
CHEMBL557478 IC50 > 100000.0 nM -
CHEMBL559642 IC50 > 10000.0 nM -
CHEMBL557479 IC50 > 10000.0 nM -
CHEMBL560156 IC50 > 10000.0 nM -
CHEMBL562929 IC50 > 10000.0 nM -
CHEMBL556391 IC50 > 10000.0 nM -
CHEMBL565035 IC50 = 111000.0 nM -
CHEMBL564559 IC50 = 229000.0 nM -
CHEMBL561637 IC50 = 184000.0 nM -
CHEMBL550139 IC50 = 418000.0 nM -
CHEMBL561498 IC50 > 1000000.0 nM -
CHEMBL551699 IC50 = 226000.0 nM -
CHEMBL562037 IC50 = 147000.0 nM -
CHEMBL562038 IC50 = 115000.0 nM -
CHEMBL549543 IC50 = 264000.0 nM -
CHEMBL561224 IC50 = 248000.0 nM -
CHEMBL556878 IC50 > 4000000.0 nM -
CHEMBL552094 IC50 > 7000000.0 nM -
CHEMBL564702 IC50 = 181000.0 nM -
CHEMBL551293 IC50 = 203000.0 nM -