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Compound Detail

CHEMBL4760718

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Cl.O=c1c2cccn2c2ccccc2n1CCCN1CCC(c2ccc(Cl)cc2)CC1

Basic Information

ChEMBL ID CHEMBL4760718
Phase Preclinical
Structure Type MOL
InChI Key UAGOSAKAAICKNK-UHFFFAOYSA-N
Parent Compound CHEMBL4803066
Active Moiety CHEMBL4803066
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
16
Publications
0
Known Names

Molecular Properties

420.0
MW (Da)
5.18
ALogP
4
HBA
0
HBD
29.6
PSA (Ų)
0.45
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H27Cl2N3O
MW 456.42
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -1.32

Activity Summary

IC50 1 meas. best 5.41

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
CX3C chemokine receptor 1
CHEMBL4843
IC50 5.41 5.41 3933.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
CX3C chemokine receptor 1 IC50 = 3932.99 nM 5.41 GPCR PRESTO-Tango dose-response in antagonist mode with target: CX3CR1 -

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL4689842 HEK-293T 346
- 10.6019/CHEMBL4689842 Fibroblast 345
- 10.6019/CHEMBL4689842 U2OS 342
- 10.6019/CHEMBL5060014 Tyrosine-protein kinase ABL1 2
- 10.6019/CHEMBL5060014 Aurora kinase A 2
- 10.6019/CHEMBL5060014 Bromodomain-containing protein 4 2
- 10.6019/CHEMBL5060014 Peregrin 2
- 10.6019/CHEMBL5060014 Cyclin-dependent kinase 2 2
- 10.6019/CHEMBL5060014 Casein kinase I isoform delta 2
- 10.6019/CHEMBL5060014 Fibroblast growth factor receptor 3 2
- 10.6019/CHEMBL5060014 Glycogen synthase kinase-3 beta 2
- 10.6019/CHEMBL5060014 Mitogen-activated protein kinase 1 2
- 10.6019/CHEMBL5060014 Transcription intermediary factor 1-alpha 2
- 10.6019/CHEMBL5724581 B cell 2
- 10.6019/CHEMBL5442687 CX3C chemokine receptor 1 1
- 10.6019/CHEMBL5724562 B cell 1

Data from ChEMBL 36 via Core Engine