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Compound Detail

CHEMBL270225

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N=C(N)NCCC[C@H](NC(=O)[C@@H]1CCN2CC[C@@](N)(Cc3ccccc3)C(=O)N12)C(=O)c1nc2ccccc2s1

Basic Information

ChEMBL ID CHEMBL270225
Phase Preclinical
Structure Type MOL
InChI Key XZWDCQQEBVTPIG-YHGPEZAFSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
2
Publications
0
Known Names

Molecular Properties

562.7
MW (Da)
1.39
ALogP
8
HBA
5
HBD
170.5
PSA (Ų)
0.11
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 C28H34N8O3S
MW 562.70
Aromatic Rings 3
Heavy Atoms 40
NP-Likeness -0.43

Activity Summary

Ki 1 meas. best 9.19

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 9.19 9.19 0.7 1

Pharmacokinetic Data

Parameter Value Units Species
F 25.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 0.65 nM 9.19 Inhibition of human alpha-thrombin 18053726

Literature References

PubMed DOI Target Context # Activities
18053726 10.1016/j.bmc.2007.11.015 Prothrombin 1
18053726 10.1016/j.bmc.2007.11.015 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine