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Compound Detail

CHEMBL18495

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Oc1ccc2c(Cc3ccc(CN4CCCC4)cc3)c(-c3ccc(OCCN4CCCC4)cc3)sc2c1

Basic Information

ChEMBL ID CHEMBL18495
Phase Preclinical
Structure Type MOL
InChI Key TYZCWXYVTGAWDO-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

512.7
MW (Da)
6.94
ALogP
5
HBA
1
HBD
35.9
PSA (Ų)
0.26
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H36N2O2S
MW 512.72
Aromatic Rings 4
Heavy Atoms 37
NP-Likeness -0.71

Activity Summary

Ki 1 meas. best 8.39

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 8.39 8.39 4.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 4.1 nM 8.39 Binding inhibition against thrombin was measured by nonlinear regression analysi... 10201846

Literature References

PubMed DOI Target Context # Activities
10201846 10.1016/s0960-894x(99)00074-8 Prothrombin 2
10201846 10.1016/s0960-894x(99)00074-8 ADMET 2
10866380 10.1016/s0960-894x(00)00211-0 Prothrombin 1
10201846 10.1016/s0960-894x(99)00074-8 NON-PROTEIN TARGET 1

Data from ChEMBL 36 via Core Engine