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Compound Detail

CHEMBL5087167

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Cn1cc2c(-c3c(-c4ccc(F)cn4)nn4c3COC(C)(C)C4)ccnc2n1

Basic Information

ChEMBL ID CHEMBL5087167
Phase Preclinical
Structure Type MOL
InChI Key MNCAUYFDXJSKPL-UHFFFAOYSA-N
4
Targets
7
Activities
2
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

378.4
MW (Da)
3.34
ALogP
7
HBA
0
HBD
70.7
PSA (Ų)
0.54
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H19FN6O
MW 378.41
Aromatic Rings 4
Heavy Atoms 28
NP-Likeness -0.82

Activity Summary

Ki 6 meas. best 5.14
IC50 1 meas. best 5.16

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H4 receptor
CHEMBL5657
IC50 5.16 5.16 6900.0 1
Sodium-dependent dopamine transporter
CHEMBL238
Ki 5.14 5.14 7216.1 2
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 5.12 5.12 7585.8 2
D(3) dopamine receptor
CHEMBL234
Ki 5.06 5.06 8625.8 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL5058645 Sodium-dependent dopamine transporter 3
- 10.6019/CHEMBL5058645 D(3) dopamine receptor 3
- 10.6019/CHEMBL5058645 5-hydroxytryptamine receptor 1A 3
- 10.6019/CHEMBL5058645 Histamine H4 receptor 2
- 10.6019/CHEMBL5058645 5-hydroxytryptamine receptor 7 1
- 10.6019/CHEMBL5058645 Beta-2 adrenergic receptor 1
- 10.6019/CHEMBL5058645 Beta-1 adrenergic receptor 1
- 10.6019/CHEMBL5058645 Histamine H2 receptor 1
- 10.6019/CHEMBL5058645 Alpha-2B adrenergic receptor 1
- 10.6019/CHEMBL5058645 Alpha-2A adrenergic receptor 1
- 10.6019/CHEMBL5058645 Alpha-1D adrenergic receptor 1
- 10.6019/CHEMBL5058645 Alpha-1B adrenergic receptor 1
- 10.6019/CHEMBL5058645 Alpha-1A adrenergic receptor 1
- 10.6019/CHEMBL5058645 5-hydroxytryptamine receptor 6 1
- 10.6019/CHEMBL5058645 5-hydroxytryptamine receptor 5A 1
- 10.6019/CHEMBL5058645 5-hydroxytryptamine receptor 3A 1
- 10.6019/CHEMBL5058645 5-hydroxytryptamine receptor 2C 1
- 10.6019/CHEMBL5058645 5-hydroxytryptamine receptor 2B 1
- 10.6019/CHEMBL5058645 5-hydroxytryptamine receptor 2A 1
- 10.6019/CHEMBL5058645 5-hydroxytryptamine receptor 1E 1

Data from ChEMBL 36 via Core Engine