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Assay Detail

CHEMBL3222928

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

Binding
Inhibition of PDGF-BB-induced Rac activation in human SMC assessed as intracellular Rac-GTP level incubated for 4 hrs prior to PDGF-BB stimulation for 2 mins by G-LISA
7
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

3-Aryl-N-aminoylsulfonylphenyl-1H-pyrazole-5-carboxamides: a new class of selective Rac inhibitors
Ferri N, Bernini SK, Corsini A, Clerici F, Erba E, Stragliotto S, Contini A
Medchemcomm (2013) 4 : 537 -541
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 4.89 5.36
Inhibition 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3218628 2 5.36
CHEMBL579882 2 5.06
CHEMBL548644 1 4.79
CHEMBL587943 1 4.72
CHEMBL3218627 1 4.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3218628 IC50 = 4400.0 nM 5.36
CHEMBL579882 IC50 = 8700.0 nM 5.06
CHEMBL548644 IC50 = 16400.0 nM 4.79
CHEMBL587943 IC50 = 19200.0 nM 4.72
CHEMBL3218627 IC50 = 29100.0 nM 4.54
CHEMBL3218628 Inhibition - % -
CHEMBL579882 Inhibition - % -