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Compound Detail

CHEMBL5592950

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CCCOc1ccc(CNC(=O)N(Cc2ccn(C)n2)[C@H]2CCN(C)CC23CC3)cc1

Basic Information

ChEMBL ID CHEMBL5592950
Phase Preclinical
Structure Type MOL
InChI Key HOVLTWZHAUDSGN-QFIPXVFZSA-N
3
Targets
3
Activities
2
Assay Types
2
PK Parameters
19
Publications
0
Known Names

Molecular Properties

425.6
MW (Da)
3.41
ALogP
5
HBA
1
HBD
62.6
PSA (Ų)
0.70
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H35N5O2
MW 425.58
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness -1.12

Activity Summary

Ki 2 meas. best 9.03
IC50 1 meas. best 5.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 9.03 9.03 0.9 1
5-hydroxytryptamine receptor 2C
CHEMBL225
Ki 8.27 8.27 5.4 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 5.05 5.05 9000.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 73.5 mL.min-1.kg-1 Rattus norvegicus
F 6.9 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
39137033 10.1021/acs.jmedchem.4c01244 ADMET 6
39137033 10.1021/acs.jmedchem.4c01244 Rattus norvegicus 2
39137033 10.1021/acs.jmedchem.4c01244 Unchecked 2
39137033 10.1021/acs.jmedchem.4c01244 Voltage-gated inwardly rectifying potassium channel KCNH2 2
39137033 10.1021/acs.jmedchem.4c01244 5-hydroxytryptamine receptor 2A 2
39137033 10.1021/acs.jmedchem.4c01244 5-hydroxytryptamine receptor 2C 2
39137033 10.1021/acs.jmedchem.4c01244 Cytochrome P450 3A4 1
39137033 10.1021/acs.jmedchem.4c01244 Cytochrome P450 2D6 1
39137033 10.1021/acs.jmedchem.4c01244 Cytochrome P450 2C9 1
39137033 10.1021/acs.jmedchem.4c01244 Cytochrome P450 2C19 1
39137033 10.1021/acs.jmedchem.4c01244 Cytochrome P450 1A2 1
39137033 10.1021/acs.jmedchem.4c01244 Alpha-2C adrenergic receptor 1
39137033 10.1021/acs.jmedchem.4c01244 Alpha-2B adrenergic receptor 1
39137033 10.1021/acs.jmedchem.4c01244 Alpha-2A adrenergic receptor 1
39137033 10.1021/acs.jmedchem.4c01244 Alpha-1A adrenergic receptor 1
39137033 10.1021/acs.jmedchem.4c01244 Histamine H1 receptor 1
39137033 10.1021/acs.jmedchem.4c01244 5-hydroxytryptamine receptor 1A 1
39137033 10.1021/acs.jmedchem.4c01244 D(2) dopamine receptor 1
39137033 10.1021/acs.jmedchem.4c01244 No relevant target 1

Data from ChEMBL 36 via Core Engine