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Compound Detail

CHEMBL5092226

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COc1ccc2c(c1)C(C(=O)N(Cc1ccc(N(C)C)cc1)c1ccc(C(C)C)cc1)CCC2.Cl

Basic Information

ChEMBL ID CHEMBL5092226
Phase Preclinical
Structure Type MOL
InChI Key UKBJWRMNGCDKNL-UHFFFAOYSA-N
Parent Compound CHEMBL1628668
Active Moiety CHEMBL1628668
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

456.6
MW (Da)
6.54
ALogP
3
HBA
0
HBD
32.8
PSA (Ų)
0.40
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H37ClN2O2
MW 493.09
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -0.83

Activity Summary

IC50 4 meas. best 6.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
C5a anaphylatoxin chemotactic receptor 1
CHEMBL2373
IC50 6.57 6.57 270.7 1
Adhesion G-protein coupled receptor F1
CHEMBL4523872
IC50 5.69 5.69 2051.5 1
Psychosine receptor
CHEMBL3714081
IC50 5.47 5.47 3350.3 1
G-protein coupled receptor 183
CHEMBL3259470
IC50 5.46 5.46 3508.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL5058577 HEK-293T 304
- 10.6019/CHEMBL5058577 U2OS 304
- 10.6019/CHEMBL5058577 Fibroblast 304
- 10.6019/CHEMBL5724801 U2OS 304
- 10.6019/CHEMBL5724801 HEK-293T 304
- 10.6019/CHEMBL5724801 Fibroblast 304
- 10.6019/CHEMBL5058564 HEK-293T 8
- 10.6019/CHEMBL5058564 U2OS 8
- 10.6019/CHEMBL5209801 Apelin receptor 2
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
- 10.6019/CHEMBL5209801 Type-1 angiotensin II receptor 2
- 10.6019/CHEMBL5209801 CX3C chemokine receptor 1 2
- 10.6019/CHEMBL5209801 Glucagon-like peptide 1 receptor 2
- 10.6019/CHEMBL5209801 Adhesion G-protein coupled receptor F1 2
- 10.6019/CHEMBL5209801 C5a anaphylatoxin chemotactic receptor 1 2
- 10.6019/CHEMBL5209801 Glucose-dependent insulinotropic receptor 2
- 10.6019/CHEMBL5209801 Beta-2 adrenergic receptor 2
- 10.6019/CHEMBL5209801 N-formyl peptide receptor 2 2
- 10.6019/CHEMBL5209801 Free fatty acid receptor 4 2
- 10.6019/CHEMBL5209801 Alpha-2A adrenergic receptor 2

Data from ChEMBL 36 via Core Engine