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Compound Detail

CHEMBL1215362

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O=C1NCc2c1cc(-c1ccnc(NC3CCCCC3)c1)nc2N1CCNCC1

Basic Information

ChEMBL ID CHEMBL1215362
Phase Preclinical
Structure Type MOL
InChI Key ORPHPLREHJAPID-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
5
PK Parameters
2
Publications
0
Known Names

Molecular Properties

392.5
MW (Da)
2.54
ALogP
6
HBA
3
HBD
82.2
PSA (Ų)
0.74
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 C22H28N6O
MW 392.51
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness -0.68

Activity Summary

IC50 1 meas. best 7.46

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase D1
CHEMBL3863
IC50 7.46 7.46 35.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 39.25 ng.hr.mL-1 Rattus norvegicus
CL 86.0 mL.min-1.kg-1 Rattus norvegicus
Cmax 31.0 nM Rattus norvegicus
F 5.0 % Rattus norvegicus
T1/2 6.2 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Serine/threonine-protein kinase D1 IC50 = 35.0 nM 7.46 Inhibition of PKD1 by TR-FRET assay 20684592

Literature References

PubMed DOI Target Context # Activities
20684592 10.1021/jm100076w Rattus norvegicus 6
20684592 10.1021/jm100076w Serine/threonine-protein kinase D1 2

Data from ChEMBL 36 via Core Engine