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Assay Detail

CHEMBL3061572

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

Binding
Antagonist activity at CCR2 (unknown origin)
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Comparative quantitative structureactivity relationship study of some 1-aminocyclopentyl-3-carboxyamides as CCR2 inhibitors using stepwise MLR, FA-MLR, and GA-PLS
Shahlaei M, Madadkar-Sobhani A, Fassihi A, Saghaie L, Shamshirian D, Sakhi H
Med Chem Res (2012) 21 : 100 -115
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 7.22 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL522688 1 8.82
CHEMBL494540 1 8.52
CHEMBL494770 1 8.34
CHEMBL523503 1 8.26
CHEMBL492569 1 8.22
CHEMBL494541 1 8.11
CHEMBL495165 1 7.66
CHEMBL492376 1 7.55
CHEMBL523054 1 7.52
CHEMBL521697 1 7.44
CHEMBL492564 1 7.29
CHEMBL495368 1 7.25
CHEMBL493780 1 7.19
CHEMBL494019 1 7.11
CHEMBL494591 1 7.07
CHEMBL494542 1 6.91
CHEMBL523857 1 6.81
CHEMBL494399 1 6.76
CHEMBL523861 1 6.73
CHEMBL493575 1 6.71
CHEMBL495151 1 6.64
CHEMBL494191 1 6.62
CHEMBL493779 1 6.44
CHEMBL524030 1 6.38
CHEMBL1187238 1 6.33
CHEMBL493843 1 6.20
CHEMBL495149 1 6.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL522688 IC50 = 1.5 nM 8.82
CHEMBL494540 IC50 = 2.999 nM 8.52
CHEMBL494770 IC50 = 4.603 nM 8.34
CHEMBL523503 IC50 = 5.495 nM 8.26
CHEMBL492569 IC50 = 5.998 nM 8.22
CHEMBL494541 IC50 = 7.798 nM 8.11
CHEMBL495165 IC50 = 21.98 nM 7.66
CHEMBL492376 IC50 = 27.99 nM 7.55
CHEMBL523054 IC50 = 29.99 nM 7.52
CHEMBL521697 IC50 = 35.97 nM 7.44
CHEMBL492564 IC50 = 51.05 nM 7.29
CHEMBL495368 IC50 = 55.98 nM 7.25
CHEMBL493780 IC50 = 63.97 nM 7.19
CHEMBL494019 IC50 = 76.91 nM 7.11
CHEMBL494591 IC50 = 84.92 nM 7.07
CHEMBL494542 IC50 = 123.03 nM 6.91
CHEMBL523857 IC50 = 155.96 nM 6.81
CHEMBL494399 IC50 = 174.98 nM 6.76
CHEMBL523861 IC50 = 187.07 nM 6.73
CHEMBL493575 IC50 = 193.2 nM 6.71
CHEMBL495151 IC50 = 230.14 nM 6.64
CHEMBL494191 IC50 = 238.78 nM 6.62
CHEMBL493779 IC50 = 362.24 nM 6.44
CHEMBL524030 IC50 = 418.79 nM 6.38
CHEMBL1187238 IC50 = 468.81 nM 6.33
CHEMBL493843 IC50 = 630.96 nM 6.20
CHEMBL495149 IC50 = 765.6 nM 6.12