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Compound Detail

CHEMBL330531

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O=C(O)CN[C@@H](C(=O)N1CCC[C@H]1C(=O)NCC#Cc1c[nH]cn1)C(c1ccccc1)c1ccccc1

Basic Information

ChEMBL ID CHEMBL330531
Phase Preclinical
Structure Type MOL
InChI Key KZEKZKWYENEHMN-JYFHCDHNSA-N
2
Targets
2
Activities
1
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

499.6
MW (Da)
1.74
ALogP
5
HBA
4
HBD
127.4
PSA (Ų)
0.33
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H29N5O4
MW 499.57
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness -0.43

Activity Summary

Ki 2 meas. best 7.36

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 7.36 7.36 44.0 1
Serine protease 1
CHEMBL3769
Ki 7.33 7.33 47.0 1

Pharmacokinetic Data

Parameter Value Units Species
Cmax 1600.0 nM Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 44.0 nM 7.36 In vitro inhibition of human thrombin. 11133089
Serine protease 1 Ki = 47.0 nM 7.33 Inhibitory activity against Bovine Trypsin 11133089

Literature References

PubMed DOI Target Context # Activities
11133089 10.1016/s0960-894x(00)00579-5 Prothrombin 1
11133089 10.1016/s0960-894x(00)00579-5 Serine protease 1 1
11133089 10.1016/s0960-894x(00)00579-5 NON-PROTEIN TARGET 1
11133089 10.1016/s0960-894x(00)00579-5 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine