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Assay Detail

CHEMBL1810320

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

Functional
Antagonist activity at human CXCR3 expressed in mouse L1.2 cells assessed as inhibition of ITAC-induced calcium mobilization by FLIPR assay
52
Total Activities
52
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type L1.2
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

Special ergolines efficiently inhibit the chemokine receptor CXCR3 in blood.
Thoma G, Baenteli R, Lewis I, Jones D, Kovarik J, Streiff MB, Zerwes HG.
Bioorg Med Chem Lett (2011) 21 : 4745 -4749
PubMed 21764306 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 52 7.40 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1809039 1 8.70
CHEMBL1809016 1 8.52
CHEMBL1809002 1 8.52
CHEMBL1809040 1 8.52
CHEMBL1809017 1 8.40
CHEMBL1806523 1 8.40
CHEMBL1809003 1 8.40
CHEMBL1809042 1 8.30
CHEMBL1809041 1 8.30
CHEMBL1809011 1 8.30
CHEMBL1809038 1 8.30
CHEMBL1809000 1 8.30
CHEMBL1809024 1 8.15
CHEMBL1809043 1 8.10
CHEMBL1809025 1 8.10
CHEMBL1808999 1 8.10
CHEMBL1808996 1 8.00
CHEMBL1809028 1 7.96
CHEMBL1808998 1 7.92
CHEMBL1809014 1 7.92
CHEMBL1809001 1 7.85
CHEMBL1809029 1 7.85
CHEMBL1809008 1 7.80
CHEMBL584554 1 7.75
CHEMBL1809015 1 7.70
CHEMBL1809013 1 7.66
CHEMBL1809019 1 7.57
CHEMBL1809037 1 7.28
CHEMBL1809018 1 7.22
CHEMBL1809010 1 7.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1809039 IC50 = 2.0 nM 8.70
CHEMBL1809016 IC50 = 3.0 nM 8.52
CHEMBL1809040 IC50 = 3.0 nM 8.52
CHEMBL1809002 IC50 = 3.0 nM 8.52
CHEMBL1809017 IC50 = 4.0 nM 8.40
CHEMBL1806523 IC50 = 4.0 nM 8.40
CHEMBL1809003 IC50 = 4.0 nM 8.40
CHEMBL1809042 IC50 = 5.0 nM 8.30
CHEMBL1809041 IC50 = 5.0 nM 8.30
CHEMBL1809011 IC50 = 5.0 nM 8.30
CHEMBL1809038 IC50 = 5.0 nM 8.30
CHEMBL1809000 IC50 = 5.0 nM 8.30
CHEMBL1809024 IC50 = 7.0 nM 8.15
CHEMBL1809025 IC50 = 8.0 nM 8.10
CHEMBL1809043 IC50 = 8.0 nM 8.10
CHEMBL1808999 IC50 = 8.0 nM 8.10
CHEMBL1808996 IC50 = 10.0 nM 8.00
CHEMBL1809028 IC50 = 11.0 nM 7.96
CHEMBL1808998 IC50 = 12.0 nM 7.92
CHEMBL1809014 IC50 = 12.0 nM 7.92
CHEMBL1809001 IC50 = 14.0 nM 7.85
CHEMBL1809029 IC50 = 14.0 nM 7.85
CHEMBL1809008 IC50 = 16.0 nM 7.80
CHEMBL584554 IC50 = 18.0 nM 7.75
CHEMBL1809015 IC50 = 20.0 nM 7.70
CHEMBL1809013 IC50 = 22.0 nM 7.66
CHEMBL1809019 IC50 = 27.0 nM 7.57
CHEMBL1809037 IC50 = 53.0 nM 7.28
CHEMBL1809018 IC50 = 60.0 nM 7.22
CHEMBL1809010 IC50 = 67.0 nM 7.17
CHEMBL1808995 IC50 = 71.0 nM 7.15
CHEMBL1809027 IC50 = 73.0 nM 7.14
CHEMBL1809005 IC50 = 74.0 nM 7.13
CHEMBL1809006 IC50 = 83.0 nM 7.08
CHEMBL1809020 IC50 = 89.0 nM 7.05
CHEMBL1809036 IC50 = 170.0 nM 6.77
CHEMBL1808997 IC50 = 187.0 nM 6.73
CHEMBL1809012 IC50 = 200.0 nM 6.70
CHEMBL1809009 IC50 = 216.0 nM 6.67
CHEMBL1809007 IC50 = 286.0 nM 6.54
CHEMBL1809004 IC50 = 457.0 nM 6.34
CHEMBL1809033 IC50 = 2200.0 nM 5.66
CHEMBL1809023 IC50 = 5400.0 nM 5.27
CHEMBL1809035 IC50 = 6120.0 nM 5.21
CHEMBL1809022 IC50 = 6200.0 nM 5.21
CHEMBL1809030 IC50 = 9475.0 nM 5.02
CHEMBL1809034 IC50 = 10000.0 nM 5.00
CHEMBL1809021 IC50 > 10000.0 nM -
CHEMBL1808994 IC50 - -
CHEMBL1809032 IC50 > 10000.0 nM -