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Compound Detail

CHEMBL101343

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N=C(N)c1ccc2c(ccn2Cc2ccccc2)c1

Basic Information

ChEMBL ID CHEMBL101343
Phase Preclinical
Structure Type MOL
InChI Key LHXHNJWJHADGSJ-UHFFFAOYSA-N
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

249.3
MW (Da)
2.97
ALogP
2
HBA
2
HBD
54.8
PSA (Ų)
0.54
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H15N3
MW 249.32
Aromatic Rings 3
Heavy Atoms 19
NP-Likeness -0.96

Activity Summary

Ki 4 meas. best 4.81

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine protease 1
CHEMBL3769
Ki 4.81 4.81 15400.0 1
Prothrombin
CHEMBL4471
Ki 4.7 4.7 20100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Serine protease 1 Ki = 15400.0 nM 4.81 Inhibition constant against bovine trypsin 6219223
Prothrombin Ki = 20100.0 nM 4.7 Inhibition constant against bovine thrombin 6219223

Literature References

PubMed DOI Target Context # Activities
6219223 10.1021/jm00356a036 Plasminogen 1
6219223 10.1021/jm00356a036 Urokinase-type plasminogen activator 1
6219223 10.1021/jm00356a036 Prothrombin 1
6219223 10.1021/jm00356a036 Serine protease 1 1
6219223 10.1021/jm00356a036 HEp-2 1

Data from ChEMBL 36 via Core Engine