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Compound Detail

CHEMBL5418259

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N[C@H]1C[C@@H](N2Cc3nn4c(C(F)(F)F)cc(C(F)(F)F)nc4c3C2)CO[C@@H]1c1cc(F)ccc1F

Basic Information

ChEMBL ID CHEMBL5418259
Phase Preclinical
Structure Type MOL
InChI Key IEWBFSLZDMTBQL-FWVNDXEPSA-N
1
Targets
1
Activities
1
Assay Types
7
PK Parameters
2
Publications
0
Known Names

Molecular Properties

507.4
MW (Da)
4.22
ALogP
6
HBA
1
HBD
68.7
PSA (Ų)
0.53
QED
1
Ro5 Violations
2
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H17F8N5O
MW 507.39
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -0.86

Activity Summary

IC50 1 meas. best 8.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 8.6 8.6 2.5 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 3700.0 ng.hr.mL-1 Rattus norvegicus
Cmax 234.53 nM Rattus norvegicus
F 71.0 % Rattus norvegicus
F 71.0 % Rattus norvegicus
T1/2 25.4 hr Rattus norvegicus
T1/2 25.4 hr Rattus norvegicus
Tmax 5.3 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 2.5 nM 8.6 Inhibition of DPP-4 (unknown origin) 37647598

Literature References

PubMed DOI Target Context # Activities
37647598 10.1021/acs.jmedchem.3c00412 ADMET 7
37647598 10.1021/acs.jmedchem.3c00412 Dipeptidyl peptidase 4 1

Data from ChEMBL 36 via Core Engine