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Assay Detail

CHEMBL979906

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

Binding
Displacement of [3H]PDBu form mouse PKCalpha by scintillation counting
ChEMBL ↗
231
Total Activities
206
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Protein kinase C alpha type (CHEMBL2567) ↗
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Conformationally constrained analogues of diacylglycerol. 29. Cells sort diacylglycerol-lactone chemical zip codes to produce diverse and selective biological activities.
Duan D, Sigano DM, Kelley JA, Lai CC, Lewin NE, Kedei N, Peach ML, Lee J, Abeyweera TP, Rotenberg SA, Kim H, Kim YH, El Kazzouli S, Chung JU, Young HA, Young MR, Baker A, Colburn NH, Haimovitz-Friedman A, Truman JP, Parrish DA, Deschamps JR, Perry NA, Surawski RJ, Blumberg PM, Marquez VE.
J Med Chem (2008) 51 : 5198 -5220
PubMed 18698758 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 231 7.23 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL527875 — — 2 8.68
CHEMBL516638 — — 2 8.61
CHEMBL472520 — — 2 8.60
CHEMBL488498 — — 2 8.57
CHEMBL488500 — — 2 8.54
CHEMBL453598 — — 2 8.53
CHEMBL488706 — — 1 8.51
CHEMBL461372 — — 2 8.47
CHEMBL511301 — — 2 8.43
CHEMBL472362 — — 1 8.31
CHEMBL358095 — — 2 8.26
CHEMBL508402 — — 1 8.10
CHEMBL471137 — — 2 8.10
CHEMBL512019 — — 1 8.07
CHEMBL461936 — — 1 8.03
CHEMBL506390 — — 1 8.00
CHEMBL461127 — — 1 7.97
CHEMBL451788 — — 2 7.96
CHEMBL472361 — — 1 7.96
CHEMBL2093989 — — 1 7.91
CHEMBL510555 — — 2 7.89
CHEMBL462377 — — 2 7.88
CHEMBL461562 — — 2 7.88
CHEMBL462136 — — 1 7.88
CHEMBL518347 — — 1 7.82
CHEMBL461563 — — 1 7.82
CHEMBL506586 — — 1 7.82
CHEMBL451802 — — 1 7.81
CHEMBL462135 — — 1 7.79
CHEMBL518503 — — 1 7.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL527875 — Ki = 2.07 nM 8.68
CHEMBL516638 — Ki = 2.45 nM 8.61
CHEMBL472520 — Ki = 2.5 nM 8.60
CHEMBL488498 — Ki = 2.66 nM 8.57
CHEMBL488500 — Ki = 2.9 nM 8.54
CHEMBL453598 — Ki = 2.96 nM 8.53
CHEMBL488706 — Ki = 3.1 nM 8.51
CHEMBL461372 — Ki = 3.38 nM 8.47
CHEMBL511301 — Ki = 3.7 nM 8.43
CHEMBL472362 — Ki = 4.89 nM 8.31
CHEMBL358095 — Ki = 5.53 nM 8.26
CHEMBL527875 — Ki = 6.1 nM 8.21
CHEMBL508402 — Ki = 7.9 nM 8.10
CHEMBL471137 — Ki = 8.0 nM 8.10
CHEMBL488498 — Ki = 8.1 nM 8.09
CHEMBL512019 — Ki = 8.5 nM 8.07
CHEMBL461936 — Ki = 9.4 nM 8.03
CHEMBL516638 — Ki = 9.3 nM 8.03
CHEMBL506390 — Ki = 10.1 nM 8.00
CHEMBL461127 — Ki = 10.7 nM 7.97
CHEMBL472361 — Ki = 11.0 nM 7.96
CHEMBL451788 — Ki = 10.9 nM 7.96
CHEMBL2093989 — Ki = 12.4 nM 7.91
CHEMBL488500 — Ki = 12.7 nM 7.90
CHEMBL510555 — Ki = 12.9 nM 7.89
CHEMBL462377 — Ki = 13.3 nM 7.88
CHEMBL461562 — Ki = 13.1 nM 7.88
CHEMBL462136 — Ki = 13.1 nM 7.88
CHEMBL461563 — Ki = 15.2 nM 7.82
CHEMBL506586 — Ki = 15.2 nM 7.82
CHEMBL518347 — Ki = 15.1 nM 7.82
CHEMBL461562 — Ki = 15.5 nM 7.81
CHEMBL451802 — Ki = 15.5 nM 7.81
CHEMBL462135 — Ki = 16.4 nM 7.79
CHEMBL518503 — Ki = 16.8 nM 7.78
CHEMBL461377 — Ki = 16.8 nM 7.78
CHEMBL453598 — Ki = 16.6 nM 7.78
CHEMBL358095 — Ki = 17.1 nM 7.77
CHEMBL461756 — Ki = 17.3 nM 7.76
CHEMBL470109 — Ki = 17.4 nM 7.76
CHEMBL461757 — Ki = 18.4 nM 7.74
CHEMBL518921 — Ki = 18.3 nM 7.74
CHEMBL462198 — Ki = 19.3 nM 7.71
CHEMBL454102 — Ki = 19.3 nM 7.71
CHEMBL451788 — Ki = 20.5 nM 7.69
CHEMBL518811 — Ki = 20.4 nM 7.69
CHEMBL461372 — Ki = 21.5 nM 7.67
CHEMBL488870 — Ki = 22.3 nM 7.65
CHEMBL487642 — Ki = 22.5 nM 7.65
CHEMBL461943 — Ki = 22.4 nM 7.65