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Compound Detail

CHEMBL233360

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N[C@H]1C[C@@H](N2CCn3c(nnc3C(F)(F)F)C2)CC[C@@H]1c1cc(F)c(F)cc1F

Basic Information

ChEMBL ID CHEMBL233360
Phase Preclinical
Structure Type MOL
InChI Key CNKRZILQBKJWDS-WMFXKJRFSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

419.4
MW (Da)
3.19
ALogP
5
HBA
1
HBD
60.0
PSA (Ų)
0.60
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H19F6N5
MW 419.37
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness -0.77

Activity Summary

IC50 3 meas. best 7.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 7.68 7.68 21.0 2
Prolyl endopeptidase FAP
CHEMBL4683
IC50 4.22 4.22 60000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 21.0 nM 7.68 Inhibition of DPP4 17502141
Dipeptidyl peptidase 4 IC50 = 21.0 nM 7.68 Inhibition of dipeptidyl peptidase 4 (unknown origin) -
Prolyl endopeptidase FAP IC50 = 60000.0 nM 4.22 Inhibition of FAP 17502141

Literature References

PubMed DOI Target Context # Activities
17502141 10.1016/j.bmcl.2007.04.106 Dipeptidyl peptidase 4 1
17502141 10.1016/j.bmcl.2007.04.106 Dipeptidyl peptidase 8 1
17502141 10.1016/j.bmcl.2007.04.106 Dipeptidyl peptidase 9 1
17502141 10.1016/j.bmcl.2007.04.106 Dipeptidyl peptidase 2 1
17502141 10.1016/j.bmcl.2007.04.106 Prolyl endopeptidase FAP 1
- 10.1007/s00044-012-0455-6 Dipeptidyl peptidase 4 1

Data from ChEMBL 36 via Core Engine