Assay Detail

CHEMBL1816013

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Functional

Antagonist activity at guinea pig CCR5 assessed as inhibition of RANTES-induced calcium mobilization

ChEMBL ↗

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Target

Unchecked (CHEMBL612545) ↗

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Primary target Unchecked

CHEMBL612545

Anchored from Assay target.

Protein identity Unchecked

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	Functional
Organism	Cavia porcellus
Confidence	0 — Uncurated / Unknown
Curated By	Autocuration

Target

Unchecked (CHEMBL612545) ↗

Type

UNCHECKED

Publication

Discovery of 4-[4-({(3R)-1-butyl-3-[(R)-cyclohexyl(hydroxy)methyl]-2,5-dioxo-1,4,9-triazaspiro[5.5]undec-9-yl}methyl)phenoxy]benzoic acid hydrochloride: a highly potent orally available CCR5 selective antagonist.

Nishizawa R, Nishiyama T, Hisaichi K, Minamoto C, Murota M, Takaoka Y, Nakai H, Tada H, Sagawa K, Shibayama S, Fukushima D, Maeda K, Mitsuya H.
Bioorg Med Chem (2011) 19 : 4028 -4042
PubMed 21658961 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	4.52	4.52

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1668019	APLAVIROC HYDROCHLORIDE	3.0	1	4.52

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1668019	APLAVIROC HYDROCHLORIDE	IC50	=	30000.0	nM	4.52