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Assay Detail

CHEMBL4669837

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Binding
Inhibition of ROCK1 (unknown origin)
4
Total Activities
4
Compounds Tested
2
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

Identification of 5H-chromeno[3,4-c]pyridine and 6H-isochromeno[3,4-c]pyridine derivatives as potent and selective dual ROCK inhibitors.
Hu Z,Wang C,Sitkoff D,Cheadle NL,Xu S,Muckelbauer JK,Adam LP,Wexler RR,Quan ML
Bioorg Med Chem Lett (2020) 30 : 127474 -127474
PubMed 32805407 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 5.74 6.85
IC50 2 6.67 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3426621 RIPASUDIL 3.0 1 7.30
CHEMBL1605605 1 6.85
CHEMBL38380 FASUDIL 3.0 1 6.03
CHEMBL2005186 BELUMOSUDIL 4.0 1 4.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3426621 RIPASUDIL IC50 = 50.0 nM 7.30
CHEMBL1605605 Ki = 140.0 nM 6.85
CHEMBL38380 FASUDIL IC50 = 940.0 nM 6.03
CHEMBL2005186 BELUMOSUDIL Ki = 24000.0 nM 4.62