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Assay Detail

CHEMBL1810317

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

Binding
Ex vivo receptor occupancy of CXCR3 in rat blood assessed as inhibition of ITAC binding after 1 hr by flow cytometry
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

C-X-C chemokine receptor type 3 (CHEMBL1075172)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 9 7.38 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1809039 1 8.30
CHEMBL1809038 1 8.15
CHEMBL1809040 1 7.85
CHEMBL1809041 1 7.80
CHEMBL1809042 1 7.64
CHEMBL1809043 1 7.40
CHEMBL1809011 1 6.39
CHEMBL1806523 1 5.48
CHEMBL1809037 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1809039 IC50 = 5.0 nM 8.30
CHEMBL1809038 IC50 = 7.0 nM 8.15
CHEMBL1809040 IC50 = 14.0 nM 7.85
CHEMBL1809041 IC50 = 16.0 nM 7.80
CHEMBL1809042 IC50 = 23.0 nM 7.64
CHEMBL1809043 IC50 = 40.0 nM 7.40
CHEMBL1809011 IC50 = 410.0 nM 6.39
CHEMBL1806523 IC50 = 3300.0 nM 5.48
CHEMBL1809037 IC50 - -