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Compound Detail

CHEMBL1204095

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COc1ccc(O)c(C(=O)c2ccc(/C=C/[C@@H]3CCCNC[C@H]3NC(=O)c3ccncc3)cc2)c1F.Cl

Basic Information

ChEMBL ID CHEMBL1204095
Phase Preclinical
Structure Type MOL
InChI Key BLLPCMVLAALVKN-ZKYKCJAYSA-N
Parent Compound CHEMBL283457
Active Moiety CHEMBL283457
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

489.6
MW (Da)
3.98
ALogP
6
HBA
3
HBD
100.5
PSA (Ų)
0.43
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H29ClFN3O4
MW 526.01
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -0.06

Activity Summary

IC50 2 meas. best 6.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
RAC-alpha serine/threonine-protein kinase
CHEMBL4282
IC50 6.8 6.8 160.0 1
cAMP-dependent protein kinase A
CHEMBL2111446
IC50 6.44 6.44 360.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
14998327 10.1021/jm0310479 RAC-alpha serine/threonine-protein kinase 1
14998327 10.1021/jm0310479 cAMP-dependent protein kinase A 1

Data from ChEMBL 36 via Core Engine