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Compound Detail

CHEMBL199925

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Nc1ccc2[nH]c(-c3ccccn3)nc2c1

Basic Information

ChEMBL ID CHEMBL199925
Phase Preclinical
Structure Type MOL
InChI Key ITFXYBZUPPBWEC-UHFFFAOYSA-N
4
Targets
7
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

210.2
MW (Da)
2.21
ALogP
3
HBA
2
HBD
67.6
PSA (Ų)
0.60
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 C12H10N4
MW 210.24
Aromatic Rings 3
Heavy Atoms 16
NP-Likeness -1.43

Activity Summary

IC50 5 meas. best 6.01
EC50 2 meas. best 4.63

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Methionine aminopeptidase
CHEMBL3423
IC50 6.01 6.01 967.0 1
Unchecked
CHEMBL612545
IC50 6.01 5.3667 970.0 3
Methionine aminopeptidase 2
CHEMBL3922
IC50 5.03 5.03 9300.0 1
Heat shock factor protein 1
CHEMBL5313
EC50 4.63 4.63 23212.0 1
Unchecked
CHEMBL612545
EC50 4.61 4.61 24607.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20621724 10.1016/j.bmcl.2010.05.093 Unchecked 3
16420038 10.1021/jm050476z Methionine aminopeptidase 2
20621724 10.1016/j.bmcl.2010.05.093 Methionine aminopeptidase 2 2
20621724 10.1016/j.bmcl.2010.05.093 Methionine aminopeptidase 1 1
38318365 10.1016/j.isci.2024.108907 Deoxynucleoside triphosphate triphosphohydrolase SAMHD1 1

Data from ChEMBL 36 via Core Engine