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Assay Detail

CHEMBL1924404

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

Binding
Displacement of [125I]CXCL10 from human CXCR3 expressed in mouse BA/F3 cells
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type BaF3
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

C-X-C chemokine receptor type 3 (CHEMBL4441)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

III. Identification of novel CXCR3 chemokine receptor antagonists with a pyrazinyl-piperazinyl-piperidine scaffold.
Kim SH, Anilkumar GN, Zawacki LG, Zeng Q, Yang DY, Shao Y, Dong G, Xu X, Yu W, Jiang Y, Jenh CH, Hall JW, Carroll CD, Hobbs DW, Baldwin JJ, McGuinness BF, Rosenblum SB, Kozlowski JA, Shankar BB, Shih NY.
Bioorg Med Chem Lett (2011) 21 : 6982 -6986
PubMed 22018463 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 40 8.59 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1921863 1 9.52
CHEMBL1921866 1 9.52
CHEMBL472288 1 9.52
CHEMBL1921865 1 9.40
CHEMBL1921858 1 9.10
CHEMBL1921864 1 9.10
CHEMBL1921879 1 9.05
CHEMBL1921868 1 9.05
CHEMBL1921891 1 8.96
CHEMBL1921878 1 8.92
CHEMBL1921896 1 8.89
CHEMBL1921871 1 8.82
CHEMBL1921883 1 8.82
CHEMBL1921877 1 8.82
CHEMBL1921884 1 8.74
CHEMBL1921869 1 8.72
CHEMBL1921861 1 8.72
CHEMBL1921882 1 8.72
CHEMBL1921887 1 8.72
CHEMBL1921890 1 8.70
CHEMBL1921886 1 8.62
CHEMBL1921876 1 8.60
CHEMBL1921880 1 8.54
CHEMBL1921881 1 8.54
CHEMBL1921875 1 8.47
CHEMBL1921889 1 8.44
CHEMBL1921859 1 8.43
CHEMBL1921885 1 8.40
CHEMBL1921874 1 8.39
CHEMBL1921895 1 8.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1921863 IC50 = 0.3 nM 9.52
CHEMBL472288 IC50 = 0.3 nM 9.52
CHEMBL1921866 IC50 = 0.3 nM 9.52
CHEMBL1921865 IC50 = 0.4 nM 9.40
CHEMBL1921858 IC50 = 0.8 nM 9.10
CHEMBL1921864 IC50 = 0.8 nM 9.10
CHEMBL1921879 IC50 = 0.9 nM 9.05
CHEMBL1921868 IC50 = 0.9 nM 9.05
CHEMBL1921891 IC50 = 1.1 nM 8.96
CHEMBL1921878 IC50 = 1.2 nM 8.92
CHEMBL1921896 IC50 = 1.3 nM 8.89
CHEMBL1921871 IC50 = 1.5 nM 8.82
CHEMBL1921877 IC50 = 1.5 nM 8.82
CHEMBL1921883 IC50 = 1.5 nM 8.82
CHEMBL1921884 IC50 = 1.8 nM 8.74
CHEMBL1921869 IC50 = 1.9 nM 8.72
CHEMBL1921887 IC50 = 1.9 nM 8.72
CHEMBL1921882 IC50 = 1.9 nM 8.72
CHEMBL1921861 IC50 = 1.9 nM 8.72
CHEMBL1921890 IC50 = 2.0 nM 8.70
CHEMBL1921886 IC50 = 2.4 nM 8.62
CHEMBL1921876 IC50 = 2.5 nM 8.60
CHEMBL1921880 IC50 = 2.9 nM 8.54
CHEMBL1921881 IC50 = 2.9 nM 8.54
CHEMBL1921875 IC50 = 3.4 nM 8.47
CHEMBL1921889 IC50 = 3.6 nM 8.44
CHEMBL1921859 IC50 = 3.7 nM 8.43
CHEMBL1921885 IC50 = 4.0 nM 8.40
CHEMBL1921874 IC50 = 4.1 nM 8.39
CHEMBL1921895 IC50 = 4.2 nM 8.38
CHEMBL1921873 IC50 = 4.4 nM 8.36
CHEMBL1921892 IC50 = 5.4 nM 8.27
CHEMBL1921870 IC50 = 6.4 nM 8.19
CHEMBL1921867 IC50 = 8.4 nM 8.08
CHEMBL1921860 IC50 = 8.5 nM 8.07
CHEMBL1921872 IC50 = 9.0 nM 8.05
CHEMBL1921888 IC50 = 18.0 nM 7.75
CHEMBL1921862 IC50 = 76.0 nM 7.12
CHEMBL1921893 IC50 = 235.0 nM 6.63
CHEMBL1921894 IC50 > 1000.0 nM -