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Compound Detail

CHEMBL270875

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NCCCn1cc(C2=C(c3c[nH]c4ccccc34)C(=O)NC2=O)c2ccccc21

Basic Information

ChEMBL ID CHEMBL270875
Phase Preclinical
Structure Type MOL
InChI Key APYXQTXFRIDSGE-UHFFFAOYSA-N
3
Targets
6
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

384.4
MW (Da)
3.04
ALogP
4
HBA
3
HBD
92.9
PSA (Ų)
0.46
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C23H20N4O2
MW 384.44
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -0.33

Activity Summary

IC50 6 meas. best 7.58

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 7.58 7.165 26.0 2
Calcium/calmodulin-dependent protein kinase type II subunit delta
CHEMBL2801
IC50 6.42 6.42 380.0 3
cAMP-dependent protein kinase (PKA)
CHEMBL2094138
IC50 6.3 6.3 500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10998351 10.1042/0264-6021:3510095 Unchecked 5
1874734 10.1016/s0021-9258(18)98476-0 Unchecked 2
10998351 10.1042/0264-6021:3510095 MAP kinase-activated protein kinase 2 1
10998351 10.1042/0264-6021:3510095 Rho-associated protein kinase 2 1
10998351 10.1042/0264-6021:3510095 Glycogen synthase kinase-3 beta 1
10998351 10.1042/0264-6021:3510095 Ribosomal protein S6 kinase beta-1 1
10998351 10.1042/0264-6021:3510095 Serine/threonine-protein kinase Sgk1 1
10998351 10.1042/0264-6021:3510095 RAC-alpha serine/threonine-protein kinase 1
10998351 10.1042/0264-6021:3510095 [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial 1
10998351 10.1042/0264-6021:3510095 Protein kinase C alpha type 1
10998351 10.1042/0264-6021:3510095 MAP kinase-activated protein kinase 5 1
10998351 10.1042/0264-6021:3510095 Ribosomal protein S6 kinase alpha-5 1
18334294 10.1016/j.bmcl.2008.02.059 Calcium/calmodulin-dependent protein kinase type II subunit delta 1
10998351 10.1042/0264-6021:3510095 Mitogen-activated protein kinase 13 1
10998351 10.1042/0264-6021:3510095 Mitogen-activated protein kinase 12 1
10998351 10.1042/0264-6021:3510095 Mitogen-activated protein kinase 11 1
10998351 10.1042/0264-6021:3510095 Mitogen-activated protein kinase 14 1
10998351 10.1042/0264-6021:3510095 Mitogen-activated protein kinase 8 1
10998351 10.1042/0264-6021:3510095 Mitogen-activated protein kinase 1 1
18337095 10.1016/j.bmcl.2008.02.057 Calcium/calmodulin-dependent protein kinase type II subunit delta 1

Data from ChEMBL 36 via Core Engine