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Assay Detail

CHEMBL1670499

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

Binding
Inhibition of PKA by RFBA assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Optimisation of 6-substituted isoquinolin-1-amine based ROCK-I inhibitors.
Ray P, Wright J, Adam J, Boucharens S, Black D, Brown AR, Epemolu O, Fletcher D, Huggett M, Jones P, Laats S, Lyons A, de Man J, Morphy R, Sherborne B, Sherry L, Straten Nv, Westwood P, York M.
Bioorg Med Chem Lett (2011) 21 : 1084 -1088
PubMed 21251828 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.71 6.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1667967 1 6.50
CHEMBL1667970 1 6.40
CHEMBL1667975 1 6.30
CHEMBL1667977 1 6.20
CHEMBL1667969 SAR-407899 FREE BASE 2.0 1 5.80
CHEMBL1667974 1 5.60
CHEMBL1667979 1 5.50
CHEMBL1667980 1 5.20
CHEMBL1667976 1 5.20
CHEMBL1667978 1 5.10
CHEMBL1667963 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1667967 IC50 = 316.23 nM 6.50
CHEMBL1667970 IC50 = 398.11 nM 6.40
CHEMBL1667975 IC50 = 501.19 nM 6.30
CHEMBL1667977 IC50 = 630.96 nM 6.20
CHEMBL1667969 SAR-407899 FREE BASE IC50 = 1584.89 nM 5.80
CHEMBL1667974 IC50 = 2511.89 nM 5.60
CHEMBL1667979 IC50 = 3162.28 nM 5.50
CHEMBL1667980 IC50 = 6309.57 nM 5.20
CHEMBL1667976 IC50 = 6309.57 nM 5.20
CHEMBL1667978 IC50 = 7943.28 nM 5.10
CHEMBL1667963 IC50 = 10000.0 nM 5.00