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Assay Detail

CHEMBL1062035

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Binding
Inhibitory constant against PKA
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

cAMP-dependent protein kinase (PKA) (CHEMBL2094138)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

The structure of dimeric ROCK I reveals the mechanism for ligand selectivity.
Jacobs M, Hayakawa K, Swenson L, Bellon S, Fleming M, Taslimi P, Doran J.
J Biol Chem (2006) 281 : 260 -268
PubMed 16249185 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 6.16 6.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL406821 1 6.47
CHEMBL38380 FASUDIL 3.0 1 6.34
CHEMBL1233300 HYDROXYFASUDIL 1 5.66
CHEMBL559147 Y-27632 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL406821 Ki = 340.0 nM 6.47
CHEMBL38380 FASUDIL Ki = 460.0 nM 6.34
CHEMBL1233300 HYDROXYFASUDIL Ki = 2200.0 nM 5.66
CHEMBL559147 Y-27632 Ki > 5000.0 nM -