Assay Detail

CHEMBL2066541

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Binding

Displacement of 5-FAM-conjugated AVP-diPhe-FAM from cIAP1 BIR3 domain after 30 mins by fluorescence polarization-based competition assay

ChEMBL ↗

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Target

Baculoviral IAP repeat-containing protein 2 (CHEMBL5462) ↗

Open DB target context

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Baculoviral IAP repeat-containing protein 2 (CHEMBL5462) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Baculoviral IAP repeat-containing protein 2

CHEMBL5462

Anchored from Assay target.

Protein identity Baculoviral IAP repeat-containing protein 2

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

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

Target

Baculoviral IAP repeat-containing protein 2 (CHEMBL5462) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).

Flygare JA, Beresini M, Budha N, Chan H, Chan IT, Cheeti S, Cohen F, Deshayes K, Doerner K, Eckhardt SG, Elliott LO, Feng B, Franklin MC, Reisner SF, Gazzard L, Halladay J, Hymowitz SG, La H, LoRusso P, Maurer B, Murray L, Plise E, Quan C, Stephan JP, Young SG, Tom J, Tsui V, Um J, Varfolomeev E, Vucic D, Wagner AJ, Wallweber HJ, Wang L, Ware J, Wen Z, Wong H, Wong JM, Wong M, Wong S, Yu R, Zobel K, Fairbrother WJ.
J Med Chem (2012) 55 : 4101 -4113
PubMed 22413863 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Ki	1	7.77	7.77

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL2063869	GDC-0152	1.0	1	7.77

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL2063869	GDC-0152	Ki	=	17.0	nM	7.77