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Compound Detail

CHEMBL120187

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COC(=O)N[C@@H](C(=O)N1CCC[C@H]1C(=O)NCc1ccc(C(=N)N)cc1)C(c1ccccc1)c1ccccc1

Basic Information

ChEMBL ID CHEMBL120187
Phase Preclinical
Structure Type MOL
InChI Key MNSLHONIQQUMSX-AZGAKELHSA-N
1
Targets
1
Activities
1
Assay Types
6
PK Parameters
5
Publications
0
Known Names

Molecular Properties

527.6
MW (Da)
3.13
ALogP
5
HBA
4
HBD
137.6
PSA (Ų)
0.25
QED
1
Ro5 Violations
9
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 -0.57

Activity Summary

Ki 1 meas. best 10.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 10.52 10.52 0.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 9900.0 ng.hr.mL-1 Rattus norvegicus
AUC 56783.33 ng.hr.mL-1 Rattus norvegicus
CL 3.0 mL.min-1.kg-1 Rattus norvegicus
Cmax 7581.07 nM Rattus norvegicus
F 6.0 % Rattus norvegicus
T1/2 1.15 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 0.03 nM 10.52 In vitro inhibition constant (Ki) against human thrombin 12904065

Literature References

PubMed DOI Target Context # Activities
12904065 10.1021/jm030025j Rattus norvegicus 9
12904065 10.1021/jm030025j ADMET 2
12904065 10.1021/jm030025j Prothrombin 1
12904065 10.1021/jm030025j Canis familiaris 1
12904065 10.1021/jm030025j Homo sapiens 1

Data from ChEMBL 36 via Core Engine