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Compound Detail

CHEMBL407631

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O=C(NCC#Cc1c[nH]cn1)[C@@H]1CCCN1C(=O)[C@H](NS(=O)(=O)Cc1ccccc1)C(c1ccccc1)c1ccccc1

Basic Information

ChEMBL ID CHEMBL407631
Phase Preclinical
Structure Type MOL
InChI Key YZCNNGYXTMBYEO-IGYGKHONSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

595.7
MW (Da)
3.19
ALogP
5
HBA
3
HBD
124.3
PSA (Ų)
0.24
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H33N5O4S
MW 595.73
Aromatic Rings 4
Heavy Atoms 43
NP-Likeness -0.78

Activity Summary

Ki 2 meas. best 8.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 8.52 8.52 3.0 1
Serine protease 1
CHEMBL3769
Ki 7.62 7.62 24.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 3.0 nM 8.52 In vitro inhibition of human thrombin. 11133089
Serine protease 1 Ki = 24.0 nM 7.62 Inhibitory activity against Bovine Trypsin 11133089

Literature References

PubMed DOI Target Context # Activities
11133089 10.1016/s0960-894x(00)00579-5 Prothrombin 1
11133089 10.1016/s0960-894x(00)00579-5 Serine protease 1 1
11133089 10.1016/s0960-894x(00)00579-5 NON-PROTEIN TARGET 1

Data from ChEMBL 36 via Core Engine