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Compound Detail

CHEMBL45480

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CCCc1ccc(NS(=O)(=O)Cc2ccccc2)c(=O)n1CC(=O)NCc1ccc(N)nc1C

Basic Information

ChEMBL ID CHEMBL45480
Phase Preclinical
Structure Type MOL
InChI Key UBCBHGGCRITWCL-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
4
PK Parameters
6
Publications
0
Known Names

Molecular Properties

483.6
MW (Da)
2.34
ALogP
7
HBA
3
HBD
136.2
PSA (Ų)
0.40
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H29N5O4S
MW 483.59
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -1.35

Activity Summary

Ki 2 meas. best 9.07

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 9.07 9.07 0.8 1
Serine protease 1
CHEMBL209
Ki 5.85 5.85 1400.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 19633.75 ng.hr.mL-1 Canis lupus familiaris
AUC 2867.69 ng.hr.mL-1 Canis lupus familiaris
Cmax 9460.0 nM Canis lupus familiaris
T1/2 189.0 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9873422 10.1016/s0960-894x(98)00297-2 Canis familiaris 6
9873422 10.1016/s0960-894x(98)00297-2 Rattus norvegicus 4
9873422 10.1016/s0960-894x(98)00297-2 ADMET 2
9873422 10.1016/s0960-894x(98)00297-2 Prothrombin 1
9873422 10.1016/s0960-894x(98)00297-2 Serine protease 1 1
9873422 10.1016/s0960-894x(98)00297-2 No relevant target 1

Data from ChEMBL 36 via Core Engine