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Compound Detail

CHEMBL289318

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Cc1cc(-c2ccccc2)ccc1C(=O)N[C@@H](CCCN=C(N)N)B1O[C@@H]2CC3CC(C3(C)C)[C@]2(C)O1

Basic Information

ChEMBL ID CHEMBL289318
Phase Preclinical
Structure Type MOL
InChI Key OBUOQQGAOGKDBP-RAWSOWQXSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

502.5
MW (Da)

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H39BN4O3
MW 502.47

Activity Summary

Ki 2 meas. best 9.38
IC50 1 meas. best 6.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
Ki 9.38 9.38 0.4 1
Serine protease 1
CHEMBL209
Ki 8.38 8.38 4.2 1
Unchecked
CHEMBL612545
IC50 6.22 6.22 600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin Ki = 0.42 nM 9.38 Inhibition of thrombin -
Serine protease 1 Ki = 4.2 nM 8.38 Inhibition of trypsin -
Unchecked IC50 = 600.0 nM 6.22 In vitro inhibitory concentration expressed as thrombin time of the compound -

Literature References

PubMed DOI Target Context # Activities
- 10.1016/S0960-894X(97)00254-0 Prothrombin 1
- 10.1016/S0960-894X(97)00254-0 Serine protease 1 1
- 10.1016/S0960-894X(97)00254-0 Unchecked 1

Data from ChEMBL 36 via Core Engine