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Compound Detail

CHEMBL5428541

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CC[C@H](N)CNc1ccnc(-c2cc(-c3cnn(C)c3)ccc2O)n1

Basic Information

ChEMBL ID CHEMBL5428541
Phase Preclinical
Structure Type MOL
InChI Key SCJXQZZYGYLKJG-AWEZNQCLSA-N
3
Targets
4
Activities
1
Assay Types
2
PK Parameters
8
Publications
0
Known Names

Molecular Properties

338.4
MW (Da)
2.40
ALogP
7
HBA
3
HBD
101.9
PSA (Ų)
0.64
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H22N6O
MW 338.42
Aromatic Rings 3
Heavy Atoms 25
NP-Likeness -1.12

Activity Summary

IC50 4 meas. best 9.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase D1
CHEMBL3863
IC50 9.0 7.11 1.0 2
Serine/threonine-protein kinase D3
CHEMBL2595
IC50 8.7 8.7 2.0 1
Serine/threonine-protein kinase D2
CHEMBL4900
IC50 8.6 8.6 2.5 1

Pharmacokinetic Data

Parameter Value Units Species
F 100.0 % Mus musculus
T1/2 1.0 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
36538005 10.1021/acs.jmedchem.2c01599 Serine/threonine-protein kinase D1 2
36538005 10.1021/acs.jmedchem.2c01599 ADMET 2
36538005 10.1021/acs.jmedchem.2c01599 Serine/threonine-protein kinase D2 1
36538005 10.1021/acs.jmedchem.2c01599 Serine/threonine-protein kinase D3 1
36538005 10.1021/acs.jmedchem.2c01599 Cyclin-dependent kinase 5 1
36538005 10.1021/acs.jmedchem.2c01599 Dual specificity tyrosine-phosphorylation-regulated kinase 2 1
36538005 10.1021/acs.jmedchem.2c01599 Serine/threonine-protein kinase pim-1 1
36538005 10.1021/acs.jmedchem.2c01599 Unchecked 1

Data from ChEMBL 36 via Core Engine