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Assay Detail

CHEMBL4233278

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

Binding
Inhibition of ROCK1 (6 to 553 residues) (unknown origin) using Lys-Lys-Arg-Asn-Arg-Thr-Leu-Ser-Val as substrate by pyruvate kinase-lactate dehydrogenase coupled assay
11
Total Activities
11
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

ROCK inhibitors 2. Improving potency, selectivity and solubility through the application of rationally designed solubilizing groups.
Gao H, Marhefka C, Jacobs MD, Cao J, Bandarage UK, Green J.
Bioorg Med Chem Lett (2018) 28 : 2616 -2621
PubMed 29945794 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.09 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4237479 1 8.00
CHEMBL4251324 1 7.89
CHEMBL4241204 1 7.35
CHEMBL4240949 1 7.33
CHEMBL4245507 1 7.29
CHEMBL3581121 1 7.08
CHEMBL4241689 1 7.06
CHEMBL4249314 1 6.66
CHEMBL4241299 1 6.62
CHEMBL4248852 1 6.37
CHEMBL4242549 1 6.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4237479 Ki = 10.0 nM 8.00
CHEMBL4251324 Ki = 13.0 nM 7.89
CHEMBL4241204 Ki = 45.0 nM 7.35
CHEMBL4240949 Ki = 47.0 nM 7.33
CHEMBL4245507 Ki = 51.0 nM 7.29
CHEMBL3581121 Ki = 83.0 nM 7.08
CHEMBL4241689 Ki = 88.0 nM 7.06
CHEMBL4249314 Ki = 220.0 nM 6.66
CHEMBL4241299 Ki = 240.0 nM 6.62
CHEMBL4248852 Ki = 430.0 nM 6.37
CHEMBL4242549 Ki = 510.0 nM 6.29