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Compound Detail

CHEMBL103581

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N[C@@H](C(=O)N1CCC[C@H]1C(=O)NCc1cc(Cl)ccc1Cl)C(c1ccccc1)c1ccccc1

Basic Information

ChEMBL ID CHEMBL103581
Phase Preclinical
Structure Type MOL
InChI Key VTUWWZYFAXSACB-UKILVPOCSA-N
1
Targets
2
Activities
1
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

496.4
MW (Da)
4.76
ALogP
3
HBA
2
HBD
75.4
PSA (Ų)
0.50
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 C27H27Cl2N3O2
MW 496.44
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -0.98

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 2

Pharmacokinetic Data

Parameter Value Units Species
F 45.0 % Canis lupus familiaris
T1/2 1.667 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 3.0 nM 8.52 Inhibitory potency against human thrombin 15163182
Prothrombin Ki = 3.0 nM 8.52 Inhibition of thrombin (unknown origin) 29072911

Literature References

PubMed DOI Target Context # Activities
15163182 10.1021/jm030303e Canis familiaris 2
15163182 10.1021/jm030303e Prothrombin 1
29072911 10.1021/acs.jmedchem.7b00772 Prothrombin 1

Data from ChEMBL 36 via Core Engine