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Assay Detail

CHEMBL1049024

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

Binding
Displacement of 125I-IP10 from recombinant human CXCR3 receptor expressed in Ba/F3 cell membrane after 1 to 4 hrs by scintillation counting
32
Total Activities
32
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 Intermediate

Target

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

Publication

Novel CXCR3 antagonists with a piperazinyl-piperidine core.
McGuinness BF, Carroll CD, Zawacki LG, Dong G, Yang C, Hobbs DW, Jacob-Samuel B, Hall JW, Jenh CH, Kozlowski JA, Anilkumar GN, Rosenblum SB.
Bioorg Med Chem Lett (2009) 19 : 5205 -5208
PubMed 19647429 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 32 6.26 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL570734 1 7.80
CHEMBL569117 1 7.50
CHEMBL578779 1 7.46
CHEMBL565760 1 7.16
CHEMBL578546 1 7.07
CHEMBL571377 1 7.07
CHEMBL565980 1 7.05
CHEMBL568676 1 6.96
CHEMBL565970 1 6.92
CHEMBL577409 1 6.85
CHEMBL568668 1 6.80
CHEMBL570356 1 6.50
CHEMBL583655 1 6.48
CHEMBL579195 1 6.43
CHEMBL565968 1 6.39
CHEMBL576841 1 6.33
CHEMBL571289 1 6.29
CHEMBL565761 1 6.25
CHEMBL583651 1 6.06
CHEMBL565559 1 5.72
CHEMBL584079 1 5.72
CHEMBL569336 1 5.70
CHEMBL570958 1 5.57
CHEMBL571467 1 5.54
CHEMBL565979 1 5.43
CHEMBL576842 1 5.42
CHEMBL587391 1 5.39
CHEMBL570509 1 5.35
CHEMBL570705 1 5.14
CHEMBL587013 1 5.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL570734 Ki = 16.0 nM 7.80
CHEMBL569117 Ki = 32.0 nM 7.50
CHEMBL578779 Ki = 35.0 nM 7.46
CHEMBL565760 Ki = 70.0 nM 7.16
CHEMBL578546 Ki = 85.0 nM 7.07
CHEMBL571377 Ki = 86.0 nM 7.07
CHEMBL565980 Ki = 90.0 nM 7.05
CHEMBL568676 Ki = 110.0 nM 6.96
CHEMBL565970 Ki = 120.0 nM 6.92
CHEMBL577409 Ki = 140.0 nM 6.85
CHEMBL568668 Ki = 160.0 nM 6.80
CHEMBL570356 Ki = 320.0 nM 6.50
CHEMBL583655 Ki = 330.0 nM 6.48
CHEMBL579195 Ki = 370.0 nM 6.43
CHEMBL565968 Ki = 410.0 nM 6.39
CHEMBL576841 Ki = 470.0 nM 6.33
CHEMBL571289 Ki = 510.0 nM 6.29
CHEMBL565761 Ki = 560.0 nM 6.25
CHEMBL583651 Ki = 870.0 nM 6.06
CHEMBL565559 Ki = 1900.0 nM 5.72
CHEMBL584079 Ki = 1900.0 nM 5.72
CHEMBL569336 Ki = 2000.0 nM 5.70
CHEMBL570958 Ki = 2700.0 nM 5.57
CHEMBL571467 Ki = 2900.0 nM 5.54
CHEMBL565979 Ki = 3700.0 nM 5.43
CHEMBL576842 Ki = 3800.0 nM 5.42
CHEMBL587391 Ki = 4100.0 nM 5.39
CHEMBL570509 Ki = 4500.0 nM 5.35
CHEMBL570705 Ki = 7200.0 nM 5.14
CHEMBL587013 Ki = 8900.0 nM 5.05
CHEMBL571815 Ki = 23000.0 nM 4.64
CHEMBL568684 Ki > 50000.0 nM -