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Compound Detail

CHEMBL154274

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COc1ccc(S(=O)(=O)Nc2cc(Br)ccc2Br)cc1N1CCNCC1

Basic Information

ChEMBL ID CHEMBL154274
Phase Preclinical
Structure Type MOL
InChI Key OCIBSJABYJIGGA-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
3
PK Parameters
15
Publications
0
Known Names

Molecular Properties

505.2
MW (Da)
3.43
ALogP
5
HBA
2
HBD
70.7
PSA (Ų)
0.65
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H19Br2N3O3S
MW 505.23
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -1.62

Activity Summary

Ki 3 meas. best 9.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 6
CHEMBL3371
Ki 9.0 9.0 1.0 1
5-hydroxytryptamine receptor 7
CHEMBL3155
Ki 8.99 8.99 1.0 1
5-hydroxytryptamine receptor 4
CHEMBL1875
Ki 5.5 5.5 3162.3 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 17.0 uM min uM-1 Rattus norvegicus
CL 43.0 mL.min-1.kg-1 Rattus norvegicus
F 20.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11140733 10.1016/s0960-894x(00)00597-7 Rattus norvegicus 4
11140733 10.1016/s0960-894x(00)00597-7 5-hydroxytryptamine receptor 6 1
11140733 10.1016/s0960-894x(00)00597-7 5-hydroxytryptamine receptor 1A 1
11140733 10.1016/s0960-894x(00)00597-7 5-hydroxytryptamine receptor 1B 1
11140733 10.1016/s0960-894x(00)00597-7 5-hydroxytryptamine receptor 1D 1
11140733 10.1016/s0960-894x(00)00597-7 5-hydroxytryptamine receptor 1E 1
11140733 10.1016/s0960-894x(00)00597-7 5-hydroxytryptamine receptor 1F 1
11140733 10.1016/s0960-894x(00)00597-7 5-hydroxytryptamine receptor 2A 1
11140733 10.1016/s0960-894x(00)00597-7 5-hydroxytryptamine receptor 2B 1
11140733 10.1016/s0960-894x(00)00597-7 5-hydroxytryptamine receptor 2C 1
11140733 10.1016/s0960-894x(00)00597-7 5-hydroxytryptamine receptor 4 1
11140733 10.1016/s0960-894x(00)00597-7 5-hydroxytryptamine receptor 7 1
11140733 10.1016/s0960-894x(00)00597-7 Alpha-1B adrenergic receptor 1
11140733 10.1016/s0960-894x(00)00597-7 D(2) dopamine receptor 1
11140733 10.1016/s0960-894x(00)00597-7 D(3) dopamine receptor 1

Data from ChEMBL 36 via Core Engine