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Compound Detail

CHEMBL384129

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Nc1noc2ccc(-n3nc(C(F)(F)F)c4c3C(=O)N(c3ccc(-c5ccccc5CN5CC[C@@H](O)C5)cc3)CN4)cc12

Basic Information

ChEMBL ID CHEMBL384129
Phase Preclinical
Structure Type MOL
InChI Key KWXHTGARBNTADQ-OAQYLSRUSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
15
Publications
0
Known Names

Molecular Properties

589.6
MW (Da)
4.88
ALogP
9
HBA
3
HBD
125.7
PSA (Ų)
0.27
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H26F3N7O3
MW 589.58
Aromatic Rings 5
Heavy Atoms 43
NP-Likeness -1.04

Activity Summary

Ki 3 meas. best 9.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor X
CHEMBL244
Ki 9.68 9.68 0.2 1
Prothrombin
CHEMBL204
Ki 6.89 6.89 130.0 1
Chymotrypsinogen B
CHEMBL4796
Ki 5.49 5.49 3240.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor X Ki = 0.21 nM 9.68 Binding affinity to human f10a 16870435
Prothrombin Ki = 130.0 nM 6.89 Binding affinity to human thrombin 16870435
Chymotrypsinogen B Ki = 3240.0 nM 5.49 Binding affinity to human chymotrypsin 16870435

Literature References

PubMed DOI Target Context # Activities
16870435 10.1016/j.bmcl.2006.07.002 Unchecked 6
16870435 10.1016/j.bmcl.2006.07.002 Coagulation factor X 2
16870435 10.1016/j.bmcl.2006.07.002 Coagulation factor IX 1
16870435 10.1016/j.bmcl.2006.07.002 Vitamin K-dependent protein C 1
16870435 10.1016/j.bmcl.2006.07.002 Trypsin 1
16870435 10.1016/j.bmcl.2006.07.002 Prothrombin 1
16870435 10.1016/j.bmcl.2006.07.002 Coagulation factor VII/tissue factor 1
16870435 10.1016/j.bmcl.2006.07.002 Plasminogen 1
16870435 10.1016/j.bmcl.2006.07.002 Urokinase-type plasminogen activator 1
16870435 10.1016/j.bmcl.2006.07.002 Chymotrypsinogen B 1
16870435 10.1016/j.bmcl.2006.07.002 Tissue-type plasminogen activator 1
16870435 10.1016/j.bmcl.2006.07.002 Thrombin and coagulation factor X 1
16870435 10.1016/j.bmcl.2006.07.002 Coagulation factor IX and X 1
16870435 10.1016/j.bmcl.2006.07.002 Coagulation factor VII and X 1
16870435 10.1016/j.bmcl.2006.07.002 Coagulation factor X and plasma kallikrein 1

Data from ChEMBL 36 via Core Engine