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Assay Detail

CHEMBL4669818

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

Binding
Inhibition of ROCK1 (unknown origin) using FITC-AHA-AKRRRLSSLRA-OH peptide substrate by caliper assay
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of a phenylpyrazole amide ROCK inhibitor as a tool molecule for in vivo studies.
Hu Z,Wang C,Glunz PW,Li J,Cheadle NL,Chen AY,Chen XQ,Myers JE,Guarino VR,Rose A,Sack JS,Sitkoff D,Taylor DS,Xu S,Yan C,Zhang H,Zhang L,Hennan J,Adam LP,Wexler RR,Quan ML
Bioorg Med Chem Lett (2020) 30 : 127495 -127495
PubMed 32798651 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 8.00 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4114628 1 9.10
CHEMBL4791701 1 9.10
CHEMBL3913336 1 9.05
CHEMBL4753754 1 8.51
CHEMBL4764401 1 8.37
CHEMBL3960736 1 8.30
CHEMBL4746508 1 8.27
CHEMBL3907133 1 8.27
CHEMBL4111518 1 8.22
CHEMBL4756156 1 8.19
CHEMBL3951271 1 8.17
CHEMBL4114533 1 8.15
CHEMBL4741358 1 8.14
CHEMBL3955445 1 8.10
CHEMBL4111655 1 8.06
CHEMBL4783577 1 8.00
CHEMBL4109840 1 8.00
CHEMBL4780269 1 7.85
CHEMBL4799221 1 7.82
CHEMBL4757844 1 7.80
CHEMBL4784425 1 7.68
CHEMBL4799704 1 7.62
CHEMBL4749675 1 7.32
CHEMBL4740106 1 7.25
CHEMBL3951573 1 6.74
CHEMBL4111347 1 5.93

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4114628 IC50 = 0.8 nM 9.10
CHEMBL4791701 IC50 = 0.8 nM 9.10
CHEMBL3913336 IC50 = 0.9 nM 9.05
CHEMBL4753754 IC50 = 3.1 nM 8.51
CHEMBL4764401 IC50 = 4.3 nM 8.37
CHEMBL3960736 IC50 = 5.0 nM 8.30
CHEMBL4746508 IC50 = 5.4 nM 8.27
CHEMBL3907133 IC50 = 5.4 nM 8.27
CHEMBL4111518 IC50 = 6.0 nM 8.22
CHEMBL4756156 IC50 = 6.4 nM 8.19
CHEMBL3951271 IC50 = 6.7 nM 8.17
CHEMBL4114533 IC50 = 7.1 nM 8.15
CHEMBL4741358 IC50 = 7.2 nM 8.14
CHEMBL3955445 IC50 = 7.9 nM 8.10
CHEMBL4111655 IC50 = 8.7 nM 8.06
CHEMBL4783577 IC50 = 10.0 nM 8.00
CHEMBL4109840 IC50 = 10.0 nM 8.00
CHEMBL4780269 IC50 = 14.0 nM 7.85
CHEMBL4799221 IC50 = 15.0 nM 7.82
CHEMBL4757844 IC50 = 16.0 nM 7.80
CHEMBL4784425 IC50 = 21.0 nM 7.68
CHEMBL4799704 IC50 = 24.0 nM 7.62
CHEMBL4749675 IC50 = 48.0 nM 7.32
CHEMBL4740106 IC50 = 56.0 nM 7.25
CHEMBL3951573 IC50 = 182.0 nM 6.74
CHEMBL4111347 IC50 = 1170.0 nM 5.93