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Compound Detail

CHEMBL54866

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COc1cc(I)cc(C(=O)NC2CC3CCCC(C2)N3Cc2ccccc2)c1OC

Basic Information

ChEMBL ID CHEMBL54866
Phase Preclinical
Structure Type MOL
InChI Key RLMCMXONOFRGMR-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

520.4
MW (Da)
4.62
ALogP
4
HBA
1
HBD
50.8
PSA (Ų)
0.57
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H29IN2O3
MW 520.41
Aromatic Rings 2
Heavy Atoms 30
NP-Likeness -0.89

Activity Summary

Ki 3 meas. best 10.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(3) dopamine receptor
CHEMBL3138
Ki 10.4 10.4 0.0 1
D(2) dopamine receptor
CHEMBL339
Ki 10.3 10.3 0.1 1
Sigma 2 receptor
CHEMBL613288
Ki 6.38 6.38 419.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11356115 10.1021/jm0100077 D(2) dopamine receptor 1
11356115 10.1021/jm0100077 D(3) dopamine receptor 1
11356115 10.1021/jm0100077 Sigma non-opioid intracellular receptor 1 1
11356115 10.1021/jm0100077 Sigma 2 receptor 1
11356115 10.1021/jm0100077 Dopamine receptor D2 and D3 1

Data from ChEMBL 36 via Core Engine