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Compound Detail

CHEMBL286720

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O=C(Cn1c(Cl)cnc(NCC(F)(F)c2cccc[n+]2[O-])c1=O)NCc1ccccc1OCC(F)(F)F

Basic Information

ChEMBL ID CHEMBL286720
Phase Preclinical
Structure Type MOL
InChI Key IGLAHUPPDPHOHX-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
5
Publications
0
Known Names

Molecular Properties

547.9
MW (Da)
2.99
ALogP
7
HBA
2
HBD
112.2
PSA (Ų)
0.23
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H19ClF5N5O4
MW 547.87
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness -1.43

Activity Summary

Ki 1 meas. best 8.74

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 8.74 8.74 1.8 1

Pharmacokinetic Data

Parameter Value Units Species
Cmax 2290.0 nM Canis lupus familiaris
T1/2 2.5 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 1.8 nM 8.74 Inhibitory activity against human thrombin 12657281

Literature References

PubMed DOI Target Context # Activities
12657281 10.1016/s0960-894x(03)00099-4 Canis familiaris 2
12657281 10.1016/s0960-894x(03)00099-4 Prothrombin 1
12657281 10.1016/s0960-894x(03)00099-4 ADMET 1
12657281 10.1016/s0960-894x(03)00099-4 Homo sapiens 1
12657281 10.1016/s0960-894x(03)00099-4 No relevant target 1

Data from ChEMBL 36 via Core Engine