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Compound Detail

CHEMBL4094913

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N#Cc1ccc(-c2nc(NCCNc3ccc([N+](=O)[O-])c(N)n3)ncc2-c2ncc[nH]2)cc1

Basic Information

ChEMBL ID CHEMBL4094913
Phase Preclinical
Structure Type MOL
InChI Key GIHBYVIOLKYZCT-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
2
Publications
0
Known Names

Molecular Properties

442.4
MW (Da)
2.81
ALogP
10
HBA
4
HBD
184.4
PSA (Ų)
0.18
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H18N10O2
MW 442.44
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -1.56

Activity Summary

IC50 1 meas. best 8.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 8.15 8.15 7.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.5 hr Rattus norvegicus
T1/2 0.5 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 7.0 nM 8.15 Inhibition of human GSK3 using biotin-CREB peptide substrate after 1 hr by scint... 29016121

Literature References

PubMed DOI Target Context # Activities
29016121 10.1021/acs.jmedchem.7b00922 Unchecked 2
29016121 10.1021/acs.jmedchem.7b00922 Liver 2

Data from ChEMBL 36 via Core Engine