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Assay Detail

CHEMBL1647669

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

Binding
Displacement of [3H]dofetilide from human ERG
6
Total Activities
6
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

Publication

Fragment-based discovery of 6-substituted isoquinolin-1-amine based ROCK-I inhibitors.
Ray P, Wright J, Adam J, Bennett J, Boucharens S, Black D, Cook A, Brown AR, Epemolu O, Fletcher D, Haunso A, Huggett M, Jones P, Laats S, Lyons A, Mestres J, de Man J, Morphy R, Rankovic Z, Sherborne B, Sherry L, van Straten N, Westwood P, Zaman GZ.
Bioorg Med Chem Lett (2011) 21 : 97 -101
PubMed 21145740 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 5.02 6.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1643574 1 6.10
CHEMBL1643361 1 5.50
CHEMBL1233300 HYDROXYFASUDIL 1 5.10
CHEMBL1643368 1 4.70
CHEMBL38380 FASUDIL 3.0 1 4.60
CHEMBL559147 Y-27632 1 4.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1643574 Ki = 794.33 nM 6.10
CHEMBL1643361 Ki = 3162.28 nM 5.50
CHEMBL1233300 HYDROXYFASUDIL Ki = 7943.28 nM 5.10
CHEMBL1643368 Ki = 19952.62 nM 4.70
CHEMBL38380 FASUDIL Ki = 25118.86 nM 4.60
CHEMBL559147 Y-27632 Ki = 79432.82 nM 4.10