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Compound Detail

CHEMBL4552037

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Cc1[nH]c2c(-c3ccccc3)c(-c3ccccc3)nn2c(=O)c1-c1ccc2ncccc2c1

Basic Information

ChEMBL ID CHEMBL4552037
Phase Preclinical
Structure Type MOL
InChI Key ZMZOMWGRJGQLDW-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
5
PK Parameters
3
Publications
0
Known Names

Molecular Properties

428.5
MW (Da)
5.88
ALogP
4
HBA
1
HBD
63.0
PSA (Ų)
0.38
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H20N4O
MW 428.50
Aromatic Rings 6
Heavy Atoms 33
NP-Likeness -0.85

Activity Summary

IC50 1 meas. best 7.01

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
S-adenosylmethionine synthase isoform type-2
CHEMBL3313835
IC50 7.01 7.01 97.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 1650000.0 hr.ng/g Mus musculus
AUC 372000.0 hr.ng/g Mus musculus
Cmax 75379.23 nM Mus musculus
Cmax 417736.29 nM Mus musculus
Fu 0.0003 - Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33829783 10.1021/acs.jmedchem.0c01895 ADMET 11
33829783 10.1021/acs.jmedchem.0c01895 S-adenosylmethionine synthase isoform type-2 2
33829783 10.1021/acs.jmedchem.0c01895 No relevant target 2

Data from ChEMBL 36 via Core Engine