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Compound Detail

CHEMBL1172520

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O=C(c1cc(Cl)ccc1-n1nccn1)N1C[C@@H]2C[C@H](C1)N(c1ncc3cc(F)ccc3n1)C2

Basic Information

ChEMBL ID CHEMBL1172520
Phase Preclinical
Structure Type MOL
InChI Key HVXSUZLOKRFHBC-KBXCAEBGSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

463.9
MW (Da)
3.35
ALogP
7
HBA
0
HBD
80.0
PSA (Ų)
0.46
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 C23H19ClFN7O
MW 463.90
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -1.64

Activity Summary

Ki 2 meas. best 9.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Orexin/Hypocretin receptor type 1
CHEMBL5113
Ki 9.4 9.4 0.4 1
Orexin receptor type 2
CHEMBL4792
Ki 9.22 9.22 0.6 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Orexin/Hypocretin receptor type 1 Ki = 0.4 nM 9.4 Binding affinity to OX1R 20610153
Orexin receptor type 2 Ki = 0.6 nM 9.22 Binding affinity to OX2R 20610153

Literature References

PubMed DOI Target Context # Activities
20610153 10.1016/j.bmcl.2010.05.047 Orexin receptor type 2 1
20610153 10.1016/j.bmcl.2010.05.047 Orexin/Hypocretin receptor type 1 1

Data from ChEMBL 36 via Core Engine