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Assay Detail

CHEMBL915971

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

Functional
Inhibition of MCP1-induced chemotaxis in U937 cells overexpressing CCR2
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type U-937
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Design and synthesis of rho kinase inhibitors (III).
Iwakubo M, Takami A, Okada Y, Kawata T, Tagami Y, Sato M, Sugiyama T, Fukushima K, Taya S, Amano M, Kaibuchi K, Iijima H.
Bioorg Med Chem (2007) 15 : 1022 -1033
PubMed 17084087 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 4.85 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL387625 1 6.00
CHEMBL387954 1 5.00
CHEMBL375556 1 4.96
CHEMBL388285 1 4.85
CHEMBL223815 1 4.85
CHEMBL223907 1 4.82
CHEMBL389926 1 4.77
CHEMBL373759 1 4.70
CHEMBL223336 1 4.66
CHEMBL225492 1 4.64
CHEMBL438783 1 4.52
CHEMBL38380 FASUDIL 3.0 1 4.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL387625 IC50 = 1000.0 nM 6.00
CHEMBL387954 IC50 = 10000.0 nM 5.00
CHEMBL375556 IC50 = 11000.0 nM 4.96
CHEMBL388285 IC50 = 14000.0 nM 4.85
CHEMBL223815 IC50 = 14000.0 nM 4.85
CHEMBL223907 IC50 = 15000.0 nM 4.82
CHEMBL389926 IC50 = 17000.0 nM 4.77
CHEMBL373759 IC50 = 20000.0 nM 4.70
CHEMBL223336 IC50 = 22000.0 nM 4.66
CHEMBL225492 IC50 = 23000.0 nM 4.64
CHEMBL438783 IC50 = 30000.0 nM 4.52
CHEMBL38380 FASUDIL IC50 = 35000.0 nM 4.46