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Compound Detail

CHEMBL2112065

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Cc1cc(N)c2ccccc2[n+]1CCCC/C=C\CCCC[n+]1c(C)cc(N)c2ccccc21.[I-].[I-]

Basic Information

ChEMBL ID CHEMBL2112065
Phase Preclinical
Structure Type MOL
InChI Key PYCLBDXZNROUIR-GSBNXNDCSA-N
Parent Compound CHEMBL2219719
Active Moiety CHEMBL2219719
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

454.7
MW (Da)
5.95
ALogP
2
HBA
2
HBD
59.8
PSA (Ų)
0.18
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H38I2N4
MW 708.47
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness 0.23

Activity Summary

IC50 1 meas. best 4.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein kinase C alpha type
CHEMBL299
IC50 4.28 4.28 52000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protein kinase C alpha type IC50 = 52000.0 nM 4.28 Inhibition of human recombinant PKCalpha 10753478

Literature References

PubMed DOI Target Context # Activities
10753478 10.1021/jm990340z Protein kinase C alpha type 1

Data from ChEMBL 36 via Core Engine