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Compound Detail

CHEMBL276928

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CN1CCC2(CC1)COc1ccc(NC(=O)N3CCC(c4c[nH]c5ccc(F)cc45)CC3)cc12

Basic Information

ChEMBL ID CHEMBL276928
Phase Preclinical
Structure Type MOL
InChI Key HIBNGDNAJQHLGU-UHFFFAOYSA-N
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

462.6
MW (Da)
5.07
ALogP
3
HBA
2
HBD
60.6
PSA (Ų)
0.56
QED
1
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H31FN4O2
MW 462.57
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -1.01

Activity Summary

IC50 3 meas. best 9.7
Kd 1 meas. best 7.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Rattus norvegicus
CHEMBL376
IC50 9.7 9.7 0.2 1
5-hydroxytryptamine receptor 1B
CHEMBL3459
IC50 7.64 7.64 23.0 1
Oryctolagus cuniculus
CHEMBL374
Kd 7.3 7.3 50.1 1
5-hydroxytryptamine receptor 1D
CHEMBL5450
IC50 6.05 6.05 900.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10737747 10.1021/jm9811054 5-hydroxytryptamine receptor 1D 1
10737747 10.1021/jm9811054 5-hydroxytryptamine receptor 1B 1
10737747 10.1021/jm9811054 5-hydroxytryptamine receptor 1A 1
10737747 10.1021/jm9811054 Rattus norvegicus 1
10737747 10.1021/jm9811054 Oryctolagus cuniculus 1
10737747 10.1021/jm9811054 Cavia porcellus 1

Data from ChEMBL 36 via Core Engine