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Compound Detail

CHEMBL5569730

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N#C[C@@H]1CC(F)(F)CN1C(=O)CNC(=O)c1ccnc2ccc(OCCCN3CCN(C(=O)CN4CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC4)CC3)cc12

Basic Information

ChEMBL ID CHEMBL5569730
Phase Preclinical
Structure Type MOL
InChI Key ICWDAESAANBIGG-LJAQVGFWSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

872.9
MW (Da)
-0.89
ALogP
14
HBA
4
HBD
243.7
PSA (Ų)
0.15
QED
2
Ro5 Violations
16
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C40H54F2N10O10
MW 872.93
Aromatic Rings 2
Heavy Atoms 62
NP-Likeness -0.91

Activity Summary

IC50 2 meas. best 9.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prolyl endopeptidase FAP
CHEMBL4683
IC50 9.68 9.68 0.2 1
Prolyl endopeptidase
CHEMBL3202
IC50 5.08 5.08 8400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prolyl endopeptidase FAP IC50 = 0.21 nM 9.68 Inhibition of FAP (unknown origin) 38656144
Prolyl endopeptidase IC50 = 8400.0 nM 5.08 Inhibition of PREP (unknown origin) 38656144

Literature References

PubMed DOI Target Context # Activities
38656144 10.1021/acs.jmedchem.3c02402 Prolyl endopeptidase FAP 1
38656144 10.1021/acs.jmedchem.3c02402 Dipeptidyl peptidase 4 1
38656144 10.1021/acs.jmedchem.3c02402 Dipeptidyl peptidase 8 1
38656144 10.1021/acs.jmedchem.3c02402 Dipeptidyl peptidase 9 1
38656144 10.1021/acs.jmedchem.3c02402 Dipeptidyl peptidase 2 1
38656144 10.1021/acs.jmedchem.3c02402 Prolyl endopeptidase 1

Data from ChEMBL 36 via Core Engine