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Compound Detail

CHEMBL5285443

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CCCc1nnsc1C(=O)Nc1nc(SCc2ccccc2)ns1

Basic Information

ChEMBL ID CHEMBL5285443
Phase Preclinical
Structure Type MOL
InChI Key QKWXOUKSWCMBBN-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
8
PK Parameters
2
Publications
0
Known Names

Molecular Properties

377.5
MW (Da)
3.89
ALogP
8
HBA
1
HBD
80.7
PSA (Ų)
0.63
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H15N5OS3
MW 377.52
Aromatic Rings 3
Heavy Atoms 24
NP-Likeness -2.49

Activity Summary

EC50 1 meas. best 7.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sulfonylurea receptor 1, Kir6.2
CHEMBL2096972
EC50 7.0 7.0 100.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 120.0 mL.min-1.kg-1 Homo sapiens
CL 1168.0 mL.min-1.kg-1 Rattus norvegicus
CL 3.02 mL.min-1.kg-1 Rattus norvegicus
Fu 0.0001 - Rattus norvegicus
Fu 0.0001 - Homo sapiens
Fu 0.0001 - Rattus norvegicus
MRT 2.12 hr Rattus norvegicus
T1/2 3.11 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
36966977 10.1016/j.bmcl.2023.129256 ADMET 10
36966977 10.1016/j.bmcl.2023.129256 Sulfonylurea receptor 1, Kir6.2 1

Data from ChEMBL 36 via Core Engine