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Assay Detail

CHEMBL5629601

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

Binding
Inhibition of PKC alpha (unknown origin) in presence of ATP at Km
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Protein kinase C alpha type (CHEMBL299)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a novel series of selective macrocyclic PKCTheta inhibitors.
Crosignani S, Campos S, Bouix-Peter C, Harris C, Talbot E, Hu H, Wang S, Maclean J, Zanelli U, Taylor S, Foote K, Hacini-Rachinel F, Nicodeme E, Julia V.
Bioorg Med Chem Lett (2024) 100 : 129630 -129630
PubMed 38307441 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 6.60 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL565612 SOTRASTAURIN 2.0 1 8.70
CHEMBL5631765 1 7.60
CHEMBL3798011 1 7.37
CHEMBL5631904 1 7.31
CHEMBL5631570 1 7.31
CHEMBL5631499 1 7.25
CHEMBL5632236 1 7.24
CHEMBL5633664 1 7.23
CHEMBL5632070 1 7.19
CHEMBL5631412 1 7.17
CHEMBL5632134 1 7.09
CHEMBL5633970 1 6.87
CHEMBL5633180 1 6.85
CHEMBL5632086 1 6.59
CHEMBL5631319 1 6.58
CHEMBL5632287 1 6.57
CHEMBL5631515 1 6.50
CHEMBL5631596 1 6.43
CHEMBL5631314 1 6.36
CHEMBL5633500 1 6.20
CHEMBL5633314 1 6.14
CHEMBL5631838 1 6.11
CHEMBL5633898 1 6.09
CHEMBL5633148 1 6.06
CHEMBL5632103 1 6.04
CHEMBL5631688 1 6.01
CHEMBL5633390 1 5.96
CHEMBL5633916 1 5.72
CHEMBL5631971 1 5.54
CHEMBL5632646 1 5.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL565612 SOTRASTAURIN IC50 = 2.0 nM 8.70
CHEMBL5631765 IC50 = 25.0 nM 7.60
CHEMBL3798011 IC50 = 43.0 nM 7.37
CHEMBL5631904 IC50 = 49.0 nM 7.31
CHEMBL5631570 IC50 = 49.0 nM 7.31
CHEMBL5631499 IC50 = 56.0 nM 7.25
CHEMBL5632236 IC50 = 57.0 nM 7.24
CHEMBL5633664 IC50 = 59.0 nM 7.23
CHEMBL5632070 IC50 = 65.0 nM 7.19
CHEMBL5631412 IC50 = 68.0 nM 7.17
CHEMBL5632134 IC50 = 82.0 nM 7.09
CHEMBL5633970 IC50 = 135.0 nM 6.87
CHEMBL5633180 IC50 = 140.0 nM 6.85
CHEMBL5632086 IC50 = 259.0 nM 6.59
CHEMBL5631319 IC50 = 260.0 nM 6.58
CHEMBL5632287 IC50 = 270.0 nM 6.57
CHEMBL5631515 IC50 = 320.0 nM 6.50
CHEMBL5631596 IC50 = 370.0 nM 6.43
CHEMBL5631314 IC50 = 440.0 nM 6.36
CHEMBL5633500 IC50 = 630.0 nM 6.20
CHEMBL5633314 IC50 = 730.0 nM 6.14
CHEMBL5631838 IC50 = 770.0 nM 6.11
CHEMBL5633898 IC50 = 820.0 nM 6.09
CHEMBL5633148 IC50 = 880.0 nM 6.06
CHEMBL5632103 IC50 = 920.0 nM 6.04
CHEMBL5631688 IC50 = 980.0 nM 6.01
CHEMBL5633390 IC50 = 1100.0 nM 5.96
CHEMBL5633916 IC50 = 1900.0 nM 5.72
CHEMBL5631971 IC50 = 2900.0 nM 5.54
CHEMBL5632646 IC50 = 4200.0 nM 5.38
CHEMBL5633746 IC50 = 8200.0 nM 5.09
CHEMBL5631811 IC50 > 10000.0 nM -
CHEMBL5632327 IC50 > 10000.0 nM -