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Compound Detail

CHEMBL3623895

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

Basic Information

ChEMBL ID CHEMBL3623895
Phase Preclinical
Structure Type MOL
InChI Key ABECVUABIRGFJZ-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
4
PK Parameters
10
Publications
0
Known Names

Molecular Properties

411.5
MW (Da)
4.32
ALogP
6
HBA
1
HBD
89.9
PSA (Ų)
0.51
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H21N5O2
MW 411.47
Aromatic Rings 4
Heavy Atoms 31
NP-Likeness -1.43

Activity Summary

IC50 2 meas. best 9.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein-serine O-palmitoleoyltransferase porcupine
CHEMBL1255163
IC50 9.96 9.96 0.1 1
Unchecked
CHEMBL612545
IC50 9.96 9.96 0.1 1

Pharmacokinetic Data

Parameter Value Units Species
CL 43.0 mL.min-1.kg-1 Homo sapiens
CL 321.0 mL.min-1.kg-1 Mus musculus
T1/2 0.6833 hr Homo sapiens
T1/2 0.3167 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 Protein-serine O-palmitoleoyltransferase porcupine 3
26455655 10.1016/j.bmc.2015.09.048 Plasma 3
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
33822624 10.1021/acs.jmedchem.0c01799 Unchecked 1
33822624 10.1021/acs.jmedchem.0c01799 No relevant target 1

Data from ChEMBL 36 via Core Engine