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Compound Detail

CHEMBL191264

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CCOC(=O)C(Cc1ccccc1)NC(=O)NN[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)c1nccs1)C(C)C

Basic Information

ChEMBL ID CHEMBL191264
Phase Preclinical
Structure Type MOL
InChI Key USHOYDAZJAGGNO-QGMKSFRFSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

721.9
MW (Da)
1.80
ALogP
10
HBA
8
HBD
229.5
PSA (Ų)
0.02
QED
2
Ro5 Violations
20
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C35H47N9O6S
MW 721.89
Aromatic Rings 3
Heavy Atoms 51
NP-Likeness -0.36

Activity Summary

IC50 3 meas. best 6.59

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor XI
CHEMBL2820
IC50 6.59 6.59 258.0 1
Prothrombin
CHEMBL204
IC50 5.68 5.68 2100.0 1
Coagulation factor X
CHEMBL244
IC50 4.84 4.84 14300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor XI IC50 = 258.0 nM 6.59 Inhibition of factor 11a 17181160
Prothrombin IC50 = 2100.0 nM 5.68 Inhibition of thrombin 17181160
Coagulation factor X IC50 = 14300.0 nM 4.84 Inhibition of factor 10a 17181160

Literature References

PubMed DOI Target Context # Activities
17181160 10.1021/jm060978s Coagulation factor XI 1
17181160 10.1021/jm060978s Coagulation factor X 1
17181160 10.1021/jm060978s Prothrombin 1

Data from ChEMBL 36 via Core Engine