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Assay Detail

CHEMBL984306

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

Binding
Promotion of flag-tagged cIAP1 degradation in human HT1080 cells assessed as decrease in cIAPI production after 3 hrs
14
Total Activities
14
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HT-1080
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Baculoviral IAP repeat-containing protein 2 (CHEMBL5462)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Degradation-promoters of cellular inhibitor of apoptosis protein 1 based on bestatin and actinonin.
Sato S, Tetsuhashi M, Sekine K, Miyachi H, Naito M, Hashimoto Y, Aoyama H.
Bioorg Med Chem (2008) 16 : 4685 -4698
PubMed 18313309 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.43 6.28
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL457292 1 6.28
CHEMBL457092 BESTATIN METHYL ESTER 1 6.16
CHEMBL458592 1 6.08
CHEMBL457093 1 5.97
CHEMBL457293 1 5.90
CHEMBL457060 1 5.81
CHEMBL458594 1 5.33
CHEMBL458777 1 5.04
CHEMBL457466 1 4.92
CHEMBL457291 1 4.70
CHEMBL458563 1 4.62
CHEMBL458564 1 4.34
CHEMBL458593 1 -
CHEMBL458586 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL457292 IC50 = 530.0 nM 6.28
CHEMBL457092 BESTATIN METHYL ESTER IC50 = 690.0 nM 6.16
CHEMBL458592 IC50 = 840.0 nM 6.08
CHEMBL457093 IC50 = 1060.0 nM 5.97
CHEMBL457293 IC50 = 1250.0 nM 5.90
CHEMBL457060 IC50 = 1540.0 nM 5.81
CHEMBL458594 IC50 = 4690.0 nM 5.33
CHEMBL458777 IC50 = 9200.0 nM 5.04
CHEMBL457466 IC50 = 12100.0 nM 4.92
CHEMBL457291 IC50 = 19900.0 nM 4.70
CHEMBL458563 IC50 = 24100.0 nM 4.62
CHEMBL458564 IC50 = 45200.0 nM 4.34
CHEMBL458593 Activity - -
CHEMBL458586 IC50 > 20000.0 nM -