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Assay Detail

CHEMBL4235452

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

Functional
Antimigratory activity in human THP1 cells assessed as inhibition of MCP-1 mediated cell migration after 1 hr by ATP luciferase based luminescence assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type THP-1
Confidence 1 — Organism
Curated By Intermediate

Target

THP-1 (CHEMBL614245)
Type CELL-LINE
Organism Homo sapiens

Publication

ROCK inhibitors 3: Design, synthesis and structure-activity relationships of 7-azaindole-based Rho kinase (ROCK) inhibitors.
Bandarage UK, Cao J, Come JH, Court JJ, Gao H, Jacobs MD, Marhefka C, Nanthakumar S, Green J.
Bioorg Med Chem Lett (2018) 28 : 2622 -2626
PubMed 30082069 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.35 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4242191 1 7.85
CHEMBL4248525 1 7.77
CHEMBL4245242 1 7.75
CHEMBL4249925 1 7.66
CHEMBL4245197 1 7.62
CHEMBL4240458 1 7.34
CHEMBL4238696 1 7.24
CHEMBL4250547 1 7.21
CHEMBL4244717 1 7.19
CHEMBL4241305 1 7.01
CHEMBL4237255 1 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4242191 IC50 = 14.0 nM 7.85
CHEMBL4248525 IC50 = 17.0 nM 7.77
CHEMBL4245242 IC50 = 18.0 nM 7.75
CHEMBL4249925 IC50 = 22.0 nM 7.66
CHEMBL4245197 IC50 = 24.0 nM 7.62
CHEMBL4240458 IC50 = 46.0 nM 7.34
CHEMBL4238696 IC50 = 58.0 nM 7.24
CHEMBL4250547 IC50 = 61.0 nM 7.21
CHEMBL4244717 IC50 = 64.0 nM 7.19
CHEMBL4241305 IC50 = 97.0 nM 7.01
CHEMBL4237255 IC50 = 580.0 nM 6.24