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Assay Detail

CHEMBL960970

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

Functional
Antagonist activity at human CCR2 receptor expressed in CHO cells by chemotaxis assay
20
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

C-C chemokine receptor type 2 (CHEMBL4015)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and structure-activity relationship of novel CCR2 antagonists.
Kothandaraman S, Donnely KL, Butora G, Jiao R, Pasternak A, Morriello GJ, Goble SD, Zhou C, Mills SG, Maccoss M, Vicario PP, Ayala JM, Demartino JA, Struthers M, Cascieri MA, Yang L.
Bioorg Med Chem Lett (2009) 19 : 1830 -1834
PubMed 19237282 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 9.24 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL494191 4 10.00
CHEMBL522688 4 9.52
CHEMBL492564 3 9.10
CHEMBL492569 1 9.00
CHEMBL494580 1 8.48
CHEMBL494540 1 8.29
CHEMBL494541 1 -
CHEMBL494542 1 -
CHEMBL523503 1 -
CHEMBL495149 1 -
CHEMBL492376 1 -
CHEMBL495151 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL494191 IC50 = 0.1 nM 10.00
CHEMBL494191 IC50 = 0.2 nM 9.70
CHEMBL494191 IC50 = 0.2 nM 9.70
CHEMBL522688 IC50 = 0.3 nM 9.52
CHEMBL522688 IC50 = 0.3 nM 9.52
CHEMBL522688 IC50 = 0.3 nM 9.52
CHEMBL492564 IC50 = 0.8 nM 9.10
CHEMBL492564 IC50 = 1.0 nM 9.00
CHEMBL492569 IC50 = 1.0 nM 9.00
CHEMBL494191 IC50 = 1.0 nM 9.00
CHEMBL494580 IC50 = 3.3 nM 8.48
CHEMBL494540 IC50 = 5.1 nM 8.29
CHEMBL494541 IC50 - -
CHEMBL494542 IC50 - -
CHEMBL523503 IC50 - -
CHEMBL495149 IC50 - -
CHEMBL492376 IC50 - -
CHEMBL495151 IC50 - -
CHEMBL522688 IC50 - -
CHEMBL492564 IC50 - -