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Compound Detail

CHEMBL1159690

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COP(O)(O)(N[C@@H](C(=O)N1CCC[C@H]1C(=O)NCc1ccc(C(=N)N)cc1)C(c1ccccc1)c1ccccc1)OC.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL1159690
Phase Preclinical
Structure Type MOL
InChI Key DULDWWUXHPMFHX-JDAAGFJYSA-N
Parent Compound CHEMBL1199309
Active Moiety CHEMBL1199309
2
Targets
2
Activities
1
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

595.6
MW (Da)
2.77
ALogP
8
HBA
6
HBD
170.2
PSA (Ų)
0.11
QED
2
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H39F3N5O8P
MW 709.66
Aromatic Rings 3
Heavy Atoms 42
NP-Likeness -0.38

Activity Summary

Ki 2 meas. best 10.36

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 10.36 10.36 0.0 1
Serine protease 1
CHEMBL3769
Ki 8.54 8.54 2.9 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 271000.0 ng.hr.mL-1 Rattus norvegicus
Cmax 6715.47 nM Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 0.044 nM 10.36 Binding affinity against human thrombin 11909707
Serine protease 1 Ki = 2.9 nM 8.54 Binding affinity against bovine trypsin 11909707

Literature References

PubMed DOI Target Context # Activities
11909707 10.1016/s0960-894x(02)00093-8 Rattus norvegicus 2
11909707 10.1016/s0960-894x(02)00093-8 Prothrombin 1
11909707 10.1016/s0960-894x(02)00093-8 Serine protease 1 1

Data from ChEMBL 36 via Core Engine