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Compound Detail

CHEMBL3972563

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Cn1c(=O)sc2ccc(-c3ccc(C[C@@H](C#N)NC(=O)[C@@H]4CNCCCO4)cc3)cc21

Basic Information

ChEMBL ID CHEMBL3972563
Phase Preclinical
Structure Type MOL
InChI Key DRQDONWWFWYTII-ICSRJNTNSA-N
2
Targets
10
Activities
1
Assay Types
8
PK Parameters
7
Publications
0
Known Names

Molecular Properties

436.5
MW (Da)
2.20
ALogP
7
HBA
2
HBD
96.2
PSA (Ų)
0.64
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H24N4O3S
MW 436.54
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -0.86

Activity Summary

IC50 10 meas. best 8.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dipeptidyl peptidase 1
CHEMBL2252
IC50 8.62 8.6044 2.4 9
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 4.64 4.64 23000.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 15.0 mL.min-1.g-1 Homo sapiens
CL - - Canis lupus familiaris
CL 3.0 mL.min-1.kg-1 Rattus norvegicus
F - % Canis lupus familiaris
F 26.0 % Rattus norvegicus
T1/2 50.0 hr -
t1/2 - - Canis lupus familiaris
T1/2 8.0 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27690432 10.1021/acs.jmedchem.6b01127 ADMET 12
27690432 10.1021/acs.jmedchem.6b01127 Molecular identity unknown 3
27690432 10.1021/acs.jmedchem.6b01127 NON-PROTEIN TARGET 3
27690432 10.1021/acs.jmedchem.6b01127 Dipeptidyl peptidase 1 2
27690432 10.1021/acs.jmedchem.6b01127 No relevant target 2
27690432 10.1021/acs.jmedchem.6b01127 Unchecked 1
27690432 10.1021/acs.jmedchem.6b01127 Voltage-gated inwardly rectifying potassium channel KCNH2 1

Data from ChEMBL 36 via Core Engine