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Assay Detail

CHEMBL1028092

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

Binding
Inhibition of human recombinant ROCK1 expressed in Sf9 cells
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Rho-associated protein kinase 1 (CHEMBL3231)
Type SINGLE PROTEIN
Organism Homo sapiens

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 26 6.73 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL521823 1 8.52
CHEMBL523695 1 8.30
CHEMBL506153 GW876790X 1 8.30
CHEMBL493911 1 8.10
CHEMBL493066 1 7.70
CHEMBL523523 1 7.70
CHEMBL493067 1 7.40
CHEMBL523057 1 6.90
CHEMBL493875 1 6.90
CHEMBL493251 1 6.80
CHEMBL1794064 GSK-561866B 1 6.70
CHEMBL450487 1 6.65
CHEMBL522351 1 6.60
CHEMBL493874 1 6.30
CHEMBL493269 1 6.30
CHEMBL453510 1 6.30
CHEMBL445180 1 6.25
CHEMBL494088 1 6.10
CHEMBL494089 GSK-690693 1.0 1 6.05
CHEMBL1794066 GSK-619487A 1 6.00
CHEMBL523859 1 5.90
CHEMBL521642 1 5.80
CHEMBL494882 1 5.70
CHEMBL1794065 GSK-554170A 1 5.60
CHEMBL494060 1 5.40
CHEMBL493250 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL521823 IC50 = 3.0 nM 8.52
CHEMBL523695 IC50 = 5.0 nM 8.30
CHEMBL506153 GW876790X IC50 = 5.0 nM 8.30
CHEMBL493911 IC50 = 8.0 nM 8.10
CHEMBL493066 IC50 = 20.0 nM 7.70
CHEMBL523523 IC50 = 20.0 nM 7.70
CHEMBL493067 IC50 = 40.0 nM 7.40
CHEMBL523057 IC50 = 126.0 nM 6.90
CHEMBL493875 IC50 = 126.0 nM 6.90
CHEMBL493251 IC50 = 158.0 nM 6.80
CHEMBL1794064 GSK-561866B IC50 = 200.0 nM 6.70
CHEMBL450487 IC50 = 224.0 nM 6.65
CHEMBL522351 IC50 = 250.0 nM 6.60
CHEMBL493874 IC50 = 501.0 nM 6.30
CHEMBL493269 IC50 = 500.0 nM 6.30
CHEMBL453510 IC50 = 500.0 nM 6.30
CHEMBL445180 IC50 = 562.0 nM 6.25
CHEMBL494088 IC50 = 790.0 nM 6.10
CHEMBL494089 GSK-690693 IC50 = 890.0 nM 6.05
CHEMBL1794066 GSK-619487A IC50 = 1000.0 nM 6.00
CHEMBL523859 IC50 = 1260.0 nM 5.90
CHEMBL521642 IC50 = 1580.0 nM 5.80
CHEMBL494882 IC50 = 1995.0 nM 5.70
CHEMBL1794065 GSK-554170A IC50 = 2510.0 nM 5.60
CHEMBL494060 IC50 = 3980.0 nM 5.40
CHEMBL493250 IC50 - -