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Assay Detail

CHEMBL1687491

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

Functional
Antagonist activity at mouse CXCR3
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

C-X-C chemokine receptor type 3 (CHEMBL5200)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

II. SAR studies of pyridyl-piperazinyl-piperidine derivatives as CXCR3 chemokine antagonists.
Shao Y, Anilkumar GN, Carroll CD, Dong G, Hall JW, Hobbs DW, Jiang Y, Jenh CH, Kim SH, Kozlowski JA, McGuinness BF, Rosenblum SB, Schulman I, Shih NY, Shu Y, Wong MK, Yu W, Zawacki LG, Zeng Q.
Bioorg Med Chem Lett (2011) 21 : 1527 -1531
PubMed 21277198 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.38 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL472288 1 9.30
CHEMBL1681882 1 8.96
CHEMBL1681849 1 8.17
CHEMBL1681848 1 7.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL472288 IC50 = 0.5 nM 9.30
CHEMBL1681882 IC50 = 1.1 nM 8.96
CHEMBL1681849 IC50 = 6.7 nM 8.17
CHEMBL1681848 IC50 = 84.0 nM 7.08