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Compound Detail

CHEMBL3415216

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CCn1c(CNc2ccc(C(=N)N)cc2F)nc2cc(C(=O)N(CCC(=O)O)c3ccc(C)cn3)ccc21

Basic Information

ChEMBL ID CHEMBL3415216
Phase Preclinical
Structure Type MOL
InChI Key YWELKWQVPBDJPT-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

517.6
MW (Da)
3.92
ALogP
7
HBA
4
HBD
150.2
PSA (Ų)
0.18
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H28FN7O3
MW 517.57
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -1.93

Activity Summary

IC50 1 meas. best 7.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
IC50 7.72 7.72 19.2 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin IC50 = 19.16 nM 7.72 Inhibition of human thrombin using Ac-FVR-AMC as substrate incubated for 10 mins... 25874337

Literature References

PubMed DOI Target Context # Activities
25874337 10.1016/j.ejmech.2015.04.012 Prothrombin 1

Data from ChEMBL 36 via Core Engine