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Assay Detail

CHEMBL832760

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

Binding
Concentration required to inhibit [125I]MCP-1 binding to Chemokine receptor 2B
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Small molecule antagonists of the CCR2b receptor. Part 2: Discovery process and initial structure-activity relationships of diamine derivatives.
Moree WJ, Kataoka K, Ramirez-Weinhouse MM, Shiota T, Imai M, Sudo M, Tsutsumi T, Endo N, Muroga Y, Hada T, Tanaka H, Morita T, Greene J, Barnum D, Saunders J, Kato Y, Myers PL, Tarby CM.
Bioorg Med Chem Lett (2004) 14 : 5413 -5416
PubMed 15454236 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 5.08 6.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL255408 1 6.75
CHEMBL365681 1 6.43
CHEMBL2096788 1 6.24
CHEMBL181432 1 6.18
CHEMBL435499 1 6.16
CHEMBL182958 1 6.15
CHEMBL2096789 1 5.92
CHEMBL365854 1 5.64
CHEMBL2448120 1 5.51
CHEMBL187469 1 5.26
CHEMBL363908 1 5.16
CHEMBL186855 1 5.13
CHEMBL362536 1 5.11
CHEMBL187476 1 4.96
CHEMBL183681 1 4.96
CHEMBL186878 1 4.85
CHEMBL362780 1 4.77
CHEMBL185518 1 4.77
CHEMBL362340 1 4.72
CHEMBL187237 1 4.66
CHEMBL446178 1 4.58
CHEMBL184240 1 4.48
CHEMBL185283 1 4.40
CHEMBL186984 1 4.39
CHEMBL188170 1 4.38
CHEMBL184220 1 4.30
CHEMBL185190 1 4.19
CHEMBL184474 1 4.18
CHEMBL364405 1 4.13
CHEMBL363994 1 4.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL255408 IC50 = 180.0 nM 6.75
CHEMBL365681 IC50 = 370.0 nM 6.43
CHEMBL2096788 IC50 = 570.0 nM 6.24
CHEMBL181432 IC50 = 660.0 nM 6.18
CHEMBL435499 IC50 = 700.0 nM 6.16
CHEMBL182958 IC50 = 710.0 nM 6.15
CHEMBL2096789 IC50 = 1200.0 nM 5.92
CHEMBL365854 IC50 = 2300.0 nM 5.64
CHEMBL2448120 IC50 = 3100.0 nM 5.51
CHEMBL187469 IC50 = 5500.0 nM 5.26
CHEMBL363908 IC50 = 6900.0 nM 5.16
CHEMBL186855 IC50 = 7400.0 nM 5.13
CHEMBL362536 IC50 = 7800.0 nM 5.11
CHEMBL187476 IC50 = 11000.0 nM 4.96
CHEMBL183681 IC50 = 11000.0 nM 4.96
CHEMBL186878 IC50 = 14000.0 nM 4.85
CHEMBL362780 IC50 = 17000.0 nM 4.77
CHEMBL185518 IC50 = 17000.0 nM 4.77
CHEMBL362340 IC50 = 19000.0 nM 4.72
CHEMBL187237 IC50 = 22000.0 nM 4.66
CHEMBL446178 IC50 = 26000.0 nM 4.58
CHEMBL184240 IC50 = 33000.0 nM 4.48
CHEMBL185283 IC50 = 40000.0 nM 4.40
CHEMBL186984 IC50 = 41000.0 nM 4.39
CHEMBL188170 IC50 = 42000.0 nM 4.38
CHEMBL184220 IC50 = 50000.0 nM 4.30
CHEMBL185190 IC50 = 64000.0 nM 4.19
CHEMBL184474 IC50 = 66000.0 nM 4.18
CHEMBL364405 IC50 = 74000.0 nM 4.13
CHEMBL363994 IC50 = 87000.0 nM 4.06