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Compound Detail

CHEMBL4167560

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COc1ccncc1C#CCN.Cl.Cl

Basic Information

ChEMBL ID CHEMBL4167560
Phase Preclinical
Structure Type MOL
InChI Key PHMMINVMDKDZGQ-UHFFFAOYSA-N
Parent Compound CHEMBL4302469
Active Moiety CHEMBL4302469
6
Targets
6
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

162.2
MW (Da)
0.40
ALogP
3
HBA
1
HBD
48.1
PSA (Ų)
0.61
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C9H12Cl2N2O
MW 235.11
Aromatic Rings 1
Heavy Atoms 12
NP-Likeness -0.13

Activity Summary

IC50 6 meas. best 5.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cytochrome P450 2A6
CHEMBL5282
IC50 5.47 5.47 3400.0 1
Cytochrome P450 2C19
CHEMBL3622
IC50 5.03 5.03 9300.0 1
Cytochrome P450 2B6
CHEMBL4729
IC50 4.96 4.96 11000.0 1
Cytochrome P450 2E1
CHEMBL5281
IC50 4.75 4.75 18000.0 1
Cytochrome P450 1A2
CHEMBL3356
IC50 4.6 4.6 25000.0 1
Cytochrome P450 2C9
CHEMBL3397
IC50 4.55 4.55 28000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29995408 10.1021/acs.jmedchem.8b00084 Unchecked 8
29995408 10.1021/acs.jmedchem.8b00084 Cytochrome P450 2A6 1
29995408 10.1021/acs.jmedchem.8b00084 Cytochrome P450 1A2 1
29995408 10.1021/acs.jmedchem.8b00084 Cytochrome P450 2B6 1
29995408 10.1021/acs.jmedchem.8b00084 Cytochrome P450 2C8 1
29995408 10.1021/acs.jmedchem.8b00084 Cytochrome P450 2C9 1
29995408 10.1021/acs.jmedchem.8b00084 Cytochrome P450 2C19 1
29995408 10.1021/acs.jmedchem.8b00084 Cytochrome P450 2D6 1
29995408 10.1021/acs.jmedchem.8b00084 Cytochrome P450 2E1 1
29995408 10.1021/acs.jmedchem.8b00084 Cytochrome P450 3A4 1

Data from ChEMBL 36 via Core Engine