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Compound Detail

CHEMBL3623875

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Cc1cc(-c2ccc(OC(=O)Nc3ccc(-c4cnccn4)cn3)cc2)ccn1

Basic Information

ChEMBL ID CHEMBL3623875
Phase Preclinical
Structure Type MOL
InChI Key AQUPHPLXUVSULY-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
8
Publications
0
Known Names

Molecular Properties

383.4
MW (Da)
4.52
ALogP
6
HBA
1
HBD
89.9
PSA (Ų)
0.56
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 C22H17N5O2
MW 383.41
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -1.20

Activity Summary

IC50 1 meas. best 9.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein-serine O-palmitoleoyltransferase porcupine
CHEMBL1255163
IC50 9.64 9.64 0.2 1

Pharmacokinetic Data

Parameter Value Units Species
CL 135.0 mL.min-1.kg-1 Homo sapiens
CL 1430.0 mL.min-1.kg-1 Mus musculus
T1/2 0.2167 hr Homo sapiens
T1/2 0.07167 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26455655 10.1016/j.bmc.2015.09.048 No relevant target 3
26455655 10.1016/j.bmc.2015.09.048 Plasma 3
26455655 10.1016/j.bmc.2015.09.048 Protein-serine O-palmitoleoyltransferase porcupine 2
26455655 10.1016/j.bmc.2015.09.048 Liver microsome 2
26455655 10.1016/j.bmc.2015.09.048 Liver 2
26455655 10.1016/j.bmc.2015.09.048 Cytochrome P450 3A4 1
26455655 10.1016/j.bmc.2015.09.048 Cytochrome P450 2D6 1
26455655 10.1016/j.bmc.2015.09.048 ADMET 1

Data from ChEMBL 36 via Core Engine