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Assay Detail

CHEMBL766516

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Binding
Binding Affinity against protein kinase C alpha
31
Total Activities
31
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 (CHEMBL299)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Conformationally constrained analogues of diacylglycerol (DAG). 16. How much structural complexity is necessary for recognition and high binding affinity to protein kinase C?
Nacro K, Bienfait B, Lee J, Han KC, Kang JH, Benzaria S, Lewin NE, Bhattacharyya DK, Blumberg PM, Marquez VE.
J Med Chem (2000) 43 : 921 -944
PubMed 10715158 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 31 7.77 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27768 1 9.70
CHEMBL111625 1 8.64
CHEMBL137288 1 8.57
CHEMBL290876 1 8.54
CHEMBL355787 1 8.46
CHEMBL3085534 1 8.46
CHEMBL172433 1 8.26
CHEMBL3085533 1 8.23
CHEMBL368346 1 8.23
CHEMBL171577 1 8.18
CHEMBL425676 1 8.14
CHEMBL173821 1 8.08
CHEMBL369061 1 8.02
CHEMBL170120 1 7.96
CHEMBL367682 1 7.96
CHEMBL172715 1 7.92
CHEMBL107614 1 7.89
CHEMBL170464 1 7.72
CHEMBL173130 1 7.70
CHEMBL173516 1 7.62
CHEMBL440555 1 7.55
CHEMBL368472 1 7.53
CHEMBL174028 1 7.29
CHEMBL175389 1 7.27
CHEMBL173241 1 7.17
CHEMBL369163 1 6.91
CHEMBL172182 1 6.86
CHEMBL173414 1 6.79
CHEMBL176579 1 6.45
CHEMBL173670 1 6.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27768 Ki = 0.2 nM 9.70
CHEMBL111625 Ki = 2.3 nM 8.64
CHEMBL137288 Ki = 2.7 nM 8.57
CHEMBL290876 Ki = 2.9 nM 8.54
CHEMBL355787 Ki = 3.5 nM 8.46
CHEMBL3085534 Ki = 3.5 nM 8.46
CHEMBL172433 Ki = 5.5 nM 8.26
CHEMBL3085533 Ki = 5.9 nM 8.23
CHEMBL368346 Ki = 5.9 nM 8.23
CHEMBL171577 Ki = 6.6 nM 8.18
CHEMBL425676 Ki = 7.3 nM 8.14
CHEMBL173821 Ki = 8.4 nM 8.08
CHEMBL369061 Ki = 9.5 nM 8.02
CHEMBL170120 Ki = 11.0 nM 7.96
CHEMBL367682 Ki = 11.0 nM 7.96
CHEMBL172715 Ki = 12.0 nM 7.92
CHEMBL107614 Ki = 13.0 nM 7.89
CHEMBL170464 Ki = 19.0 nM 7.72
CHEMBL173130 Ki = 20.0 nM 7.70
CHEMBL173516 Ki = 24.0 nM 7.62
CHEMBL440555 Ki = 28.0 nM 7.55
CHEMBL368472 Ki = 29.5 nM 7.53
CHEMBL174028 Ki = 51.0 nM 7.29
CHEMBL175389 Ki = 54.0 nM 7.27
CHEMBL173241 Ki = 68.0 nM 7.17
CHEMBL369163 Ki = 123.0 nM 6.91
CHEMBL172182 Ki = 138.0 nM 6.86
CHEMBL173414 Ki = 164.0 nM 6.79
CHEMBL176579 Ki = 359.0 nM 6.45
CHEMBL173670 Ki = 390.0 nM 6.41
CHEMBL369665 Ki = 409.0 nM 6.39