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Compound Detail

CHEMBL379834

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COc1ccccc1Oc1cccc(CN2CCC(NC(=O)C3(c4ccccc4)CCNCC3)(C(=O)O)CC2)c1

Basic Information

ChEMBL ID CHEMBL379834
Phase Preclinical
Structure Type MOL
InChI Key TUFFUEHRXNGQLP-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

543.7
MW (Da)
4.34
ALogP
6
HBA
3
HBD
100.1
PSA (Ų)
0.37
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H37N3O5
MW 543.66
Aromatic Rings 3
Heavy Atoms 40
NP-Likeness -0.58

Activity Summary

Ki 1 meas. best 7.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
C-C chemokine receptor type 8
CHEMBL4596
Ki 7.22 7.22 60.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
C-C chemokine receptor type 8 Ki = 60.0 nM 7.22 Displacement of [125I]I309 from human CCR8 expressed in L1.2 cells 16640325

Literature References

PubMed DOI Target Context # Activities
16640325 10.1021/jm050965z C-C chemokine receptor type 8 1
16640325 10.1021/jm050965z Voltage-gated inwardly rectifying potassium channel KCNH2 1
16640325 10.1021/jm050965z Cytochrome P450 3A4 1

Data from ChEMBL 36 via Core Engine