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Compound Detail

CHEMBL4161777

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Cl.Cl.Cl.Cl.NCC#Cc1cnccc1-c1cncnc1

Basic Information

ChEMBL ID CHEMBL4161777
Phase Preclinical
Structure Type MOL
InChI Key OMRBQKCXYKBYSV-UHFFFAOYSA-N
Parent Compound CHEMBL4301668
Active Moiety CHEMBL4301668
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
11
Publications
0
Known Names

Molecular Properties

210.2
MW (Da)
0.85
ALogP
4
HBA
1
HBD
64.7
PSA (Ų)
0.71
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 C12H14Cl4N4
MW 356.08
Aromatic Rings 2
Heavy Atoms 16
NP-Likeness -0.47

Activity Summary

IC50 1 meas. best 5.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cytochrome P450 2A6
CHEMBL5282
IC50 5.57 5.57 2700.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 2.0 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cytochrome P450 2A6 IC50 = 2700.0 nM 5.57 Inhibition of CYP2A6 in human liver microsomes using coumarin as substrate prein... 29995408

Literature References

PubMed DOI Target Context # Activities
29995408 10.1021/acs.jmedchem.8b00084 Unchecked 8
29995408 10.1021/acs.jmedchem.8b00084 Cytochrome P450 1A2 1
29995408 10.1021/acs.jmedchem.8b00084 Cytochrome P450 2A6 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
29995408 10.1021/acs.jmedchem.8b00084 ADMET 1

Data from ChEMBL 36 via Core Engine