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Compound Detail

CHEMBL121379

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COC(=O)N[C@@H](C(=O)N1CCC[C@H]1C(=O)NCc1csc(C(=N)N)c1)C(c1ccccc1)c1ccccc1

Basic Information

ChEMBL ID CHEMBL121379
Phase Preclinical
Structure Type MOL
InChI Key JIOYYUTWFZPXGR-XUZZJYLKSA-N
1
Targets
1
Activities
1
Assay Types
6
PK Parameters
5
Publications
0
Known Names

Molecular Properties

533.6
MW (Da)
3.20
ALogP
6
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 C28H31N5O4S
MW 533.65
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness -0.76

Activity Summary

Ki 1 meas. best 9.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 9.22 9.22 0.6 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 21616.67 ng.hr.mL-1 Rattus norvegicus
AUC 102316.67 ng.hr.mL-1 Rattus norvegicus
CL 1.7 mL.min-1.kg-1 Rattus norvegicus
Cmax 16115.43 nM Rattus norvegicus
F 7.0 % Rattus norvegicus
T1/2 0.75 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 0.6 nM 9.22 In vitro inhibition constant (Ki) against human thrombin 12904065

Literature References

PubMed DOI Target Context # Activities
12904065 10.1021/jm030025j Rattus norvegicus 11
12904065 10.1021/jm030025j ADMET 3
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