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Assay Detail

CHEMBL863246

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

Functional
Antagonistic activity at mouse CCR1 in CHO-K1 cells
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Expert

Target

C-C chemokine receptor type 1 (CHEMBL3872)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis.
Revesz L, Bollbuck B, Buhl T, Eder J, Esser R, Feifel R, Heng R, Hiestand P, Jachez-Demange B, Loetscher P, Sparrer H, Schlapbach A, Waelchli R.
Bioorg Med Chem Lett (2005) 15 : 5160 -5164
PubMed 16198561 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 6.32 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL372807 1 8.40
CHEMBL200242 1 7.40
CHEMBL200629 1 7.30
CHEMBL200680 1 7.30
CHEMBL196860 1 6.52
CHEMBL198852 1 6.35
CHEMBL370596 1 6.30
CHEMBL198949 1 6.24
CHEMBL197375 1 6.22
CHEMBL199412 1 6.00
CHEMBL535607 BX 471 2.0 1 5.82
CHEMBL370162 1 5.52
CHEMBL200794 1 5.52
CHEMBL198966 1 5.32
CHEMBL197345 1 4.64
CHEMBL371248 1 -
CHEMBL380568 1 -
CHEMBL381446 1 -
CHEMBL381223 1 -
CHEMBL196908 1 -
CHEMBL370447 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL372807 IC50 = 4.0 nM 8.40
CHEMBL200242 IC50 = 40.0 nM 7.40
CHEMBL200629 IC50 = 50.0 nM 7.30
CHEMBL200680 IC50 = 50.0 nM 7.30
CHEMBL196860 IC50 = 300.0 nM 6.52
CHEMBL198852 IC50 = 448.0 nM 6.35
CHEMBL370596 IC50 = 500.0 nM 6.30
CHEMBL198949 IC50 = 580.0 nM 6.24
CHEMBL197375 IC50 = 600.0 nM 6.22
CHEMBL199412 IC50 = 1000.0 nM 6.00
CHEMBL535607 BX 471 IC50 = 1500.0 nM 5.82
CHEMBL370162 IC50 = 3000.0 nM 5.52
CHEMBL200794 IC50 = 3000.0 nM 5.52
CHEMBL198966 IC50 = 4800.0 nM 5.32
CHEMBL197345 IC50 = 23000.0 nM 4.64
CHEMBL371248 IC50 - -
CHEMBL380568 IC50 - -
CHEMBL381446 IC50 - -
CHEMBL381223 IC50 - -
CHEMBL196908 IC50 - -
CHEMBL370447 IC50 - -