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Assay Detail

CHEMBL768513

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

Binding
Tested for ability to displace [20e3] phorbol 12,13- dibutyrate binding from recombinant bovine Protein kinase C alpha in presence of [Ca2+]
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Protein kinase C alpha type (CHEMBL2213)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

New bivalent PKC ligands linked by a carbon spacer: enhancement in binding affinity.
Sridhar J, Wei ZL, Nowak I, Lewin NE, Ayres JA, Pearce LV, Blumberg PM, Kozikowski AP.
J Med Chem (2003) 46 : 4196 -4204
PubMed 12954072 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 6.94 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL334853 1 8.74
CHEMBL132720 1 8.62
CHEMBL337834 1 8.44
CHEMBL133853 1 8.25
CHEMBL132612 1 7.42
CHEMBL135611 1 7.25
CHEMBL336963 1 6.81
CHEMBL134413 1 6.77
CHEMBL339383 1 6.76
CHEMBL337522 1 6.68
CHEMBL334195 1 6.65
CHEMBL134287 1 6.59
CHEMBL448101 1 6.56
CHEMBL132525 1 6.53
CHEMBL133777 1 6.53
CHEMBL335486 1 6.50
CHEMBL134690 1 6.25
CHEMBL132714 1 5.35
CHEMBL334451 1 5.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL334853 Ki = 1.82 nM 8.74
CHEMBL132720 Ki = 2.39 nM 8.62
CHEMBL337834 Ki = 3.67 nM 8.44
CHEMBL133853 Ki = 5.63 nM 8.25
CHEMBL132612 Ki = 37.9 nM 7.42
CHEMBL135611 Ki = 56.6 nM 7.25
CHEMBL336963 Ki = 154.0 nM 6.81
CHEMBL134413 Ki = 169.0 nM 6.77
CHEMBL339383 Ki = 174.0 nM 6.76
CHEMBL337522 Ki = 208.0 nM 6.68
CHEMBL334195 Ki = 225.0 nM 6.65
CHEMBL134287 Ki = 254.0 nM 6.59
CHEMBL448101 Ki = 278.0 nM 6.56
CHEMBL132525 Ki = 296.0 nM 6.53
CHEMBL133777 Ki = 296.0 nM 6.53
CHEMBL335486 Ki = 320.0 nM 6.50
CHEMBL134690 Ki = 558.0 nM 6.25
CHEMBL132714 Ki = 4470.0 nM 5.35
CHEMBL334451 Ki = 7860.0 nM 5.11