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Assay Detail

CHEMBL1028095

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

Binding
Inhibition of rat ROCK1
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Rho-associated protein kinase 1 (CHEMBL5509)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Identification of 4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a novel inhibitor of AKT kinase.
Heerding DA, Rhodes N, Leber JD, Clark TJ, Keenan RM, Lafrance LV, Li M, Safonov IG, Takata DT, Venslavsky JW, Yamashita DS, Choudhry AE, Copeland RA, Lai Z, Schaber MD, Tummino PJ, Strum SL, Wood ER, Duckett DR, Eberwein D, Knick VB, Lansing TJ, McConnell RT, Zhang S, Minthorn EA, Concha NO, Warren GL, Kumar R.
J Med Chem (2008) 51 : 5663 -5679
PubMed 18800763 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.82 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL494662 1 8.22
CHEMBL188434 1 7.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL494662 IC50 = 6.0 nM 8.22
CHEMBL188434 IC50 = 38.0 nM 7.42