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Assay Detail

CHEMBL904869

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Functional
Selectivity index, ratio of IC50 for human RPTEC cells to IC50 for HT29 cells
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type RPTEC
Confidence 1 — Organism
Curated By Autocuration

Target

RPTEC (CHEMBL614883)
Type CELL-LINE
Organism Homo sapiens

Publication

Rationally designed high-affinity 2-amino-6-halopurine heat shock protein 90 inhibitors that exhibit potent antitumor activity.
Kasibhatla SR, Hong K, Biamonte MA, Busch DJ, Karjian PL, Sensintaffar JL, Kamal A, Lough RE, Brekken J, Lundgren K, Grecko R, Timony GA, Ran Y, Mansfield R, Fritz LC, Ulm E, Burrows FJ, Boehm MF.
J Med Chem (2007) 50 : 2767 -2778
PubMed 17488003 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 4.95 5.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL557165 1 5.30
CHEMBL389164 1 5.16
CHEMBL229943 1 5.00
CHEMBL229891 1 5.00
CHEMBL229577 1 4.92
CHEMBL109480 TANESPIMYCIN 3.0 1 4.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL557165 IC50 = 5000.0 nM 5.30
CHEMBL389164 IC50 = 7000.0 nM 5.16
CHEMBL229943 IC50 = 10000.0 nM 5.00
CHEMBL229891 IC50 = 10000.0 nM 5.00
CHEMBL229577 IC50 = 12000.0 nM 4.92
CHEMBL109480 TANESPIMYCIN IC50 = 50000.0 nM 4.30