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Compound Detail

CHEMBL1650431

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N#Cc1cc(F)ccc1Cn1c(N2CCC[C@@H](N)C2)ncc(F)c1=O

Basic Information

ChEMBL ID CHEMBL1650431
Phase Preclinical
Structure Type MOL
InChI Key BWZLUCZZHLODDA-CQSZACIVSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

345.4
MW (Da)
1.37
ALogP
6
HBA
1
HBD
87.9
PSA (Ų)
0.91
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H17F2N5O
MW 345.35
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness -1.53

Activity Summary

IC50 1 meas. best 6.37

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 4
CHEMBL284
IC50 6.37 6.37 430.0 1

Pharmacokinetic Data

Parameter Value Units Species
t1/2 - - Homo sapiens
t1/2 - - Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Dipeptidyl peptidase 4 IC50 = 430.0 nM 6.37 Inhibition of human DPP4 21186796

Literature References

PubMed DOI Target Context # Activities
21186796 10.1021/jm101016w Liver microsomes 2
21186796 10.1021/jm101016w Dipeptidyl peptidase 8 1
21186796 10.1021/jm101016w Dipeptidyl peptidase 4 1

Data from ChEMBL 36 via Core Engine