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Compound Detail

CHEMBL517689

5-(3-METHYL-1-TRIAZENO)IMIDAZOLE-4-CARBOXAMIDE
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Nc1c(-c2ccccc2)nc2ccccc2c1C(=O)N[C@H](c1ccccc1)C1CC1

Basic Information

ChEMBL ID CHEMBL517689
Name 5-(3-METHYL-1-TRIAZENO)IMIDAZOLE-4-CARBOXAMIDE
Phase Preclinical
Structure Type MOL
InChI Key IJZKXXAVXWWWOP-XMMPIXPASA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
3
Publications
0
Known Names

Molecular Properties

393.5
MW (Da)
5.37
ALogP
3
HBA
2
HBD
68.0
PSA (Ų)
0.48
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H23N3O
MW 393.49
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -0.74

Activity Summary

Ki 1 meas. best 8.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neuromedin-K receptor
CHEMBL4429
Ki 8.3 8.3 5.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 539.0 ng.hr/g Rattus norvegicus
Cmax 104.0 ng/g Rattus norvegicus
T1/2 0.1333 hr -

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Neuromedin-K receptor Ki = 5.012 nM 8.3 Binding affinity to NK3 receptor 19117759

Literature References

PubMed DOI Target Context # Activities
19117759 10.1016/j.bmcl.2008.12.005 Brain 2
19117759 10.1016/j.bmcl.2008.12.005 Neuromedin-K receptor 1
23895620 10.1021/jm401121k No relevant target 1

Data from ChEMBL 36 via Core Engine