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Compound Detail

CHEMBL412546

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CC(C)[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)N[C@H](C)c1ccc(Br)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)c1nccs1

Basic Information

ChEMBL ID CHEMBL412546
Phase Preclinical
Structure Type MOL
InChI Key RXTVQIZDVTYZLH-DLMOMKDTSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

752.7
MW (Da)
4.13
ALogP
7
HBA
8
HBD
207.0
PSA (Ų)
0.04
QED
2
Ro5 Violations
16
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H42BrN9O4S
MW 752.74
Aromatic Rings 4
Heavy Atoms 49
NP-Likeness -0.51

Activity Summary

IC50 3 meas. best 7.54

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Coagulation factor XI
CHEMBL2820
IC50 7.54 7.54 29.0 1
Prothrombin
CHEMBL204
IC50 6.15 6.15 710.0 1
Coagulation factor X
CHEMBL244
IC50 5.68 5.68 2100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Coagulation factor XI IC50 = 29.0 nM 7.54 Inhibition of factor 11a 17181160
Prothrombin IC50 = 710.0 nM 6.15 Inhibition of thrombin 17181160
Coagulation factor X IC50 = 2100.0 nM 5.68 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