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Compound Detail

CHEMBL422314

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Clc1ccccc1CCN1CCN(c2[nH]nc3c2CCc2ccccc2-3)CC1

Basic Information

ChEMBL ID CHEMBL422314
Phase Preclinical
Structure Type MOL
InChI Key DBPSAINLCKSSJL-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
5
Publications
0
Known Names

Molecular Properties

392.9
MW (Da)
4.19
ALogP
3
HBA
1
HBD
35.2
PSA (Ų)
0.72
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H25ClN4
MW 392.93
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -1.29

Activity Summary

Ki 1 meas. best 8.37

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(4) dopamine receptor
CHEMBL219
Ki 8.37 8.37 4.3 1

Pharmacokinetic Data

Parameter Value Units Species
F 31.0 % Rattus norvegicus
T1/2 1.0 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
D(4) dopamine receptor Ki = 4.3 nM 8.37 Binding affinity towards human dopamine receptor D4 11170639

Literature References

PubMed DOI Target Context # Activities
11170639 10.1021/jm0002432 D(4) dopamine receptor 1
11170639 10.1021/jm0002432 ADMET 1
11170639 10.1021/jm0002432 Rattus norvegicus 1
11170639 10.1021/jm0002432 Voltage-gated L-type calcium channel 1
11170639 10.1021/jm0002432 Unchecked 1

Data from ChEMBL 36 via Core Engine