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Compound Detail

CHEMBL174008

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COC(=O)/C=C/c1cn(CC(=O)N2CCC(Cc3ccccc3)CC2)c2ccc(C(=N)N)cc12

Basic Information

ChEMBL ID CHEMBL174008
Phase Preclinical
Structure Type MOL
InChI Key GJAVWABPSVJBPB-CSKARUKUSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

458.6
MW (Da)
3.59
ALogP
5
HBA
2
HBD
101.4
PSA (Ų)
0.24
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H30N4O3
MW 458.56
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -0.74

Activity Summary

Ki 3 meas. best 7.55

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 7.55 7.55 28.0 1
Serine protease 1
CHEMBL209
Ki 6.55 6.55 280.0 1
Unchecked
CHEMBL612545
Ki 5.92 5.92 1200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 28.0 nM 7.55 Inhibition of Coagulation factor II 10230612
Serine protease 1 Ki = 280.0 nM 6.55 Inhibitory activity against trypsin 10230612
Unchecked Ki = 1200.0 nM 5.92 Inhibition of factor Xa 10230612

Literature References

PubMed DOI Target Context # Activities
10230612 10.1016/s0960-894x(99)00113-4 Prothrombin 1
10230612 10.1016/s0960-894x(99)00113-4 Serine protease 1 1
10230612 10.1016/s0960-894x(99)00113-4 Unchecked 1

Data from ChEMBL 36 via Core Engine