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Compound Detail

CHEMBL83437

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N=C(N)N1CCCC(C[C@H](NC(=O)CN2C(=O)CN(CCCc3ccccc3)C(=O)[C@H]2Cc2ccccc2)C(=O)N2CCCCC2)C1

Basic Information

ChEMBL ID CHEMBL83437
Phase Preclinical
Structure Type MOL
InChI Key ZRCOHDOAWXKMSA-CJZYSFCQSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

643.8
MW (Da)
2.39
ALogP
5
HBA
3
HBD
143.1
PSA (Ų)
0.24
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C36H49N7O4
MW 643.83
Aromatic Rings 2
Heavy Atoms 47
NP-Likeness -0.52

Activity Summary

IC50 1 meas. best 5.18
Ki 1 meas. best 6.08

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 6.08 6.08 825.0 1
Prothrombin
CHEMBL204
IC50 5.18 5.18 6600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 825.0 nM 6.08 Inhibition of thrombin 10498197
Prothrombin IC50 = 6600.0 nM 5.18 Inhibitory concentration required against thrombin was determined 10498197

Literature References

PubMed DOI Target Context # Activities
10498197 10.1016/s0960-894x(99)00419-9 Prothrombin 2
10498197 10.1016/s0960-894x(99)00419-9 Serine protease 1 1

Data from ChEMBL 36 via Core Engine