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Assay Detail

CHEMBL768365

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

Binding
Inhibition of protein kinase A (PKA) in bovine heart
5
Total Activities
5
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

Inhibitors of protein kinase C. 2. Substituted bisindolylmaleimides with improved potency and selectivity.
Davis PD, Elliott LH, Harris W, Hill CH, Hurst SA, Keech E, Kumar MK, Lawton G, Nixon JS, Wilkinson SE.
J Med Chem (1992) 35 : 994 -1001
PubMed 1552513 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.44 6.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6291 BISINDOLYLMALEIMIDE IX 1 6.05
CHEMBL268888 1 5.57
CHEMBL6274 1 5.34
CHEMBL6279 1 5.31
CHEMBL267126 1 4.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6291 BISINDOLYLMALEIMIDE IX IC50 = 900.0 nM 6.05
CHEMBL268888 IC50 = 2700.0 nM 5.57
CHEMBL6274 IC50 = 4600.0 nM 5.34
CHEMBL6279 IC50 = 4900.0 nM 5.31
CHEMBL267126 IC50 = 12100.0 nM 4.92