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Compound Detail

CHEMBL372585

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CN(C)CC1CCn2c(c(C3=C(c4c[nH]c5ccccc45)C(=O)NC3=O)c3ccccc32)C1

Basic Information

ChEMBL ID CHEMBL372585
Phase Preclinical
Structure Type MOL
InChI Key KAUXQCPPAWLYAB-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

438.5
MW (Da)
3.81
ALogP
4
HBA
2
HBD
70.1
PSA (Ų)
0.48
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H26N4O2
MW 438.53
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -0.13

Activity Summary

Kd 1 meas. best 6.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase pim-1
CHEMBL2147
Kd 6.6 6.6 250.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Serine/threonine-protein kinase pim-1 Kd = 250.0 nM 6.6 Binding affinity to non phosphorylated PIM1 16302800

Literature References

PubMed DOI Target Context # Activities
16302800 10.1021/jm0504858 Serine/threonine-protein kinase pim-1 4
18077363 10.1073/pnas.0708800104 Serine/threonine-protein kinase 26 2
18077363 10.1073/pnas.0708800104 Ribosomal protein S6 kinase alpha-3 2
18077363 10.1073/pnas.0708800104 Cyclin-dependent kinase 2 1
18077363 10.1073/pnas.0708800104 Casein kinase I isoform gamma-2 1
18077363 10.1073/pnas.0708800104 Casein kinase I isoform gamma-1 1
18077363 10.1073/pnas.0708800104 Serine/threonine-protein kinase 25 1
18077363 10.1073/pnas.0708800104 Dual specificity protein kinase CLK2 1
18077363 10.1073/pnas.0708800104 Dual specificity protein kinase CLK1 1
18077363 10.1073/pnas.0708800104 Serine/threonine-protein kinase Chk2 1
18077363 10.1073/pnas.0708800104 Cyclin-dependent kinase-like 1 1
18077363 10.1073/pnas.0708800104 Cyclin-dependent kinase 6 1
18077363 10.1073/pnas.0708800104 Calcium/calmodulin-dependent protein kinase kinase 2 1
18077363 10.1073/pnas.0708800104 Calcium/calmodulin-dependent protein kinase type IV 1
18077363 10.1073/pnas.0708800104 Calcium/calmodulin-dependent protein kinase type II subunit gamma 1
18077363 10.1073/pnas.0708800104 Calcium/calmodulin-dependent protein kinase type II subunit delta 1
18077363 10.1073/pnas.0708800104 Calcium/calmodulin-dependent protein kinase type II subunit beta 1
18077363 10.1073/pnas.0708800104 Calcium/calmodulin-dependent protein kinase type II subunit alpha 1
18077363 10.1073/pnas.0708800104 Calcium/calmodulin-dependent protein kinase type 1G 1
18077363 10.1073/pnas.0708800104 Calcium/calmodulin-dependent protein kinase type 1D 1

Data from ChEMBL 36 via Core Engine