Assay Detail

CHEMBL1695217

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Functional

Antagonist activity at CCR5 assessed as inhibition of intracellular calcium mobilization

ChEMBL ↗

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Target

C-C chemokine receptor type 5 (CHEMBL274) ↗

Open DB target context

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C-C chemokine receptor type 5 (CHEMBL274) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target C-C chemokine receptor type 5

CHEMBL274

Anchored from Assay target.

Protein identity C-C chemokine receptor type 5

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
Confidence	8 — Homologous single protein target
Curated By	Autocuration

Target

C-C chemokine receptor type 5 (CHEMBL274) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery of INCB9471, a Potent, Selective, and Orally Bioavailable CCR5 Antagonist with Potent Anti-HIV-1 Activity.

Xue CB, Chen L, Cao G, Zhang K, Wang A, Meloni D, Glenn J, Anand R, Xia M, Kong L, Huang T, Feng H, Zheng C, Li M, Galya L, Zhou J, Shin N, Baribaud F, Solomon K, Scherle P, Zhao B, Diamond S, Emm T, Keller D, Contel N, Yeleswaram S, Vaddi K, Hollis G, Newton R, Friedman S, Metcalf B.
ACS Med Chem Lett (2010) 1 : 483 -487
PubMed 24900235 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	7.80	7.80

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1688243	INCB-9471	2.0	1	7.80

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1688243	INCB-9471	IC50	=	16.0	nM	7.80