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Assay Detail

CHEMBL761887

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Binding
Inhibition of protein kinase A was evaluated as Inhibitory concentration
22
Total Activities
22
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. 3. Potent and highly selective bisindolylmaleimides by conformational restriction.
Bit RA, Davis PD, Elliott LH, Harris W, Hill CH, Keech E, Kumar H, Lawton G, Maw A, Nixon JS.
J Med Chem (1993) 36 : 21 -29
PubMed 8421286 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 5.25 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388978 STAUROSPORINE 1 6.92
CHEMBL319788 1 6.05
CHEMBL99825 1 5.96
CHEMBL96002 1 5.62
CHEMBL327723 1 5.58
CHEMBL421565 1 5.55
CHEMBL100084 1 5.50
CHEMBL330160 1 5.48
CHEMBL316918 1 5.41
CHEMBL328399 1 5.39
CHEMBL1202928 1 5.35
CHEMBL1202926 1 5.32
CHEMBL269264 1 5.28
CHEMBL1202927 1 5.07
CHEMBL317961 1 4.92
CHEMBL97522 1 4.89
CHEMBL95592 1 4.64
CHEMBL317792 1 4.62
CHEMBL95613 1 4.47
CHEMBL317987 1 4.17
CHEMBL327509 1 4.03
CHEMBL319787 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388978 STAUROSPORINE IC50 = 121.0 nM 6.92
CHEMBL319788 IC50 = 900.0 nM 6.05
CHEMBL99825 IC50 = 1100.0 nM 5.96
CHEMBL96002 IC50 = 2400.0 nM 5.62
CHEMBL327723 IC50 = 2600.0 nM 5.58
CHEMBL421565 IC50 = 2800.0 nM 5.55
CHEMBL100084 IC50 = 3200.0 nM 5.50
CHEMBL330160 IC50 = 3300.0 nM 5.48
CHEMBL316918 IC50 = 3900.0 nM 5.41
CHEMBL328399 IC50 = 4100.0 nM 5.39
CHEMBL1202928 IC50 = 4500.0 nM 5.35
CHEMBL1202926 IC50 = 4800.0 nM 5.32
CHEMBL269264 IC50 = 5200.0 nM 5.28
CHEMBL1202927 IC50 = 8600.0 nM 5.07
CHEMBL317961 IC50 = 12100.0 nM 4.92
CHEMBL97522 IC50 = 12800.0 nM 4.89
CHEMBL95592 IC50 = 23000.0 nM 4.64
CHEMBL317792 IC50 = 24000.0 nM 4.62
CHEMBL95613 IC50 = 34000.0 nM 4.47
CHEMBL317987 IC50 = 68000.0 nM 4.17
CHEMBL327509 IC50 = 92500.0 nM 4.03
CHEMBL319787 IC50 > 100000.0 nM -