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Compound Detail

CHEMBL566522

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Fc1ccc2c(c1)nc(N1CCN(Cc3c[nH]cn3)CC1)c1cccn12

Basic Information

ChEMBL ID CHEMBL566522
Phase Preclinical
Structure Type MOL
InChI Key BRNJLENJYHXKEL-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
12
Publications
0
Known Names

Molecular Properties

350.4
MW (Da)
2.67
ALogP
5
HBA
1
HBD
52.5
PSA (Ų)
0.62
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 C19H19FN6
MW 350.40
Aromatic Rings 4
Heavy Atoms 26
NP-Likeness -1.87

Activity Summary

IC50 1 meas. best 6.57
Ki 1 meas. best 9.17

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 3A
CHEMBL2411
Ki 9.17 9.17 0.7 1
5-hydroxytryptamine receptor 3A
CHEMBL3666
IC50 6.57 6.57 270.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19831400 10.1021/jm901126m Rattus norvegicus 12
19831400 10.1021/jm901126m Brain 3
19831400 10.1021/jm901126m ADMET 3
19831400 10.1021/jm901126m 5-hydroxytryptamine receptor 3A 2
19831400 10.1021/jm901126m 5-hydroxytryptamine receptor 1A 1
19831400 10.1021/jm901126m 5-hydroxytryptamine receptor 2A 1
19831400 10.1021/jm901126m 5-hydroxytryptamine receptor 4 1
19831400 10.1021/jm901126m Adrenergic receptor alpha-1 1
19831400 10.1021/jm901126m Alpha-2A adrenergic receptor 1
19831400 10.1021/jm901126m D(1A) dopamine receptor 1
19831400 10.1021/jm901126m D(2) dopamine receptor 1
19831400 10.1021/jm901126m Muscarinic acetylcholine receptor 1

Data from ChEMBL 36 via Core Engine