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Compound Detail

CHEMBL5633370

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Cc1ccc(-n2nccn2)c(C(=O)N[C@H]2CCC[C@@H]2Nc2cnc3ccccc3n2)c1

Basic Information

ChEMBL ID CHEMBL5633370
Phase Preclinical
Structure Type MOL
InChI Key GYTNAVCPRBXIHQ-PMACEKPBSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
3
Publications
0
Known Names

Molecular Properties

413.5
MW (Da)
3.28
ALogP
7
HBA
2
HBD
97.6
PSA (Ų)
0.52
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H23N7O
MW 413.49
Aromatic Rings 4
Heavy Atoms 31
NP-Likeness -1.27

Activity Summary

IC50 1 meas. best 7.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Orexin/Hypocretin receptor type 1
CHEMBL5113
IC50 7.8 7.8 16.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 24.0 mL.min-1.g-1 Homo sapiens
CL 335.0 mL.min-1.g-1 Rattus norvegicus
CL 442.0 mL.min-1.g-1 Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
38295907 10.1016/j.bmcl.2024.129629 ADMET 3
38295907 10.1016/j.bmcl.2024.129629 Orexin/Hypocretin receptor type 1 1
38295907 10.1016/j.bmcl.2024.129629 Orexin receptor type 2 1

Data from ChEMBL 36 via Core Engine