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Compound Detail

CHEMBL330949

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N=C(N)c1ccc(CNC(=O)[C@@H]2CCCN2C(=O)[C@H](NCC(=O)O)C(c2ccccc2)c2ccccc2)cc1

Basic Information

ChEMBL ID CHEMBL330949
Phase Preclinical
Structure Type MOL
InChI Key ZJLAXTDVOPOJCG-RPLLCQBOSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
5
Publications
0
Known Names

Molecular Properties

527.6
MW (Da)
2.45
ALogP
5
HBA
5
HBD
148.6
PSA (Ų)
0.19
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H33N5O4
MW 527.63
Aromatic Rings 3
Heavy Atoms 39
NP-Likeness -0.40

Activity Summary

Ki 1 meas. best 10.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 10.89 10.89 0.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 2000.0 ng.hr.mL-1 Rattus norvegicus
Cmax 2463.85 nM Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 0.013 nM 10.89 In vitro inhibition constant (Ki) against human thrombin 12904065

Literature References

PubMed DOI Target Context # Activities
12904065 10.1021/jm030025j Rattus norvegicus 3
12904065 10.1021/jm030025j Prothrombin 1
12904065 10.1021/jm030025j Canis familiaris 1
12904065 10.1021/jm030025j ADMET 1
12904065 10.1021/jm030025j Homo sapiens 1

Data from ChEMBL 36 via Core Engine