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Compound Detail

CHEMBL363548

CHLOROHALOPERIDOL
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O=C(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)c1ccc(Cl)cc1

Basic Information

ChEMBL ID CHEMBL363548
Name CHLOROHALOPERIDOL
Phase Preclinical
Structure Type MOL
InChI Key QETRGFJTEVVJTC-UHFFFAOYSA-N
4
Targets
6
Activities
3
Assay Types
2
PK Parameters
17
Publications
0
Known Names

Molecular Properties

392.3
MW (Da)
4.94
ALogP
3
HBA
1
HBD
40.5
PSA (Ų)
0.71
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H23Cl2NO2
MW 392.33
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -0.60

Activity Summary

Ki 4 meas. best 8.3
IC50 1 meas. best 5.29
Kd 1 meas. best 8.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(2) dopamine receptor
CHEMBL217
Kd 8.3 8.3 5.0 1
D(2) dopamine receptor
CHEMBL217
Ki 8.3 7.51 5.0 2
Alpha-1A adrenergic receptor
CHEMBL229
Ki 6.82 6.82 150.0 1
Melanin-concentrating hormone receptor 1
CHEMBL1075228
Ki 6.46 6.46 350.0 1
N-acetyltransferase Eis
CHEMBL3879870
IC50 5.29 5.29 5100.0 1

Pharmacokinetic Data

Parameter Value Units Species
Ka 1.38 10'8/M/min Homo sapiens
T1/2 0.01667 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31580666 10.1021/acs.jmedchem.9b00864 D(2) dopamine receptor 7
34825186 10.1039/D1MD00239B Mycobacterium tuberculosis variant bovis 4
34825186 10.1039/D1MD00239B Mycolicibacterium smegmatis 4
34825186 10.1039/D1MD00239B Mycobacteroides abscessus 4
34825186 10.1039/D1MD00239B Mycobacterium intracellulare 4
34825186 10.1039/D1MD00239B Mycobacterium avium 4
34825186 10.1039/D1MD00239B Mycobacterium tuberculosis 3
34825186 10.1039/D1MD00239B Unchecked 2
34825186 10.1039/D1MD00239B J774.A1 1
15267235 10.1021/jm040762v Melanin-concentrating hormone receptor 1 1
34825186 10.1039/D1MD00239B A549 1
34825186 10.1039/D1MD00239B HEK293 1
34825186 10.1039/D1MD00239B Aminoglycoside 2'-N-acetyltransferase 1
34825186 10.1039/D1MD00239B N-acetyltransferase Eis 1
17668922 10.1021/jm060383x D(2) dopamine receptor 1
17668922 10.1021/jm060383x Alpha-1A adrenergic receptor 1
17668922 10.1021/jm060383x Melanin-concentrating hormone receptor 1 1

Data from ChEMBL 36 via Core Engine