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Compound Detail

CHEMBL5090952

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Cc1ccc(C(=O)O)cc1N1CCN(c2c(C)n[nH]c2C)CC1

Basic Information

ChEMBL ID CHEMBL5090952
Phase Preclinical
Structure Type MOL
InChI Key FSSNALBCZQRFIJ-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
9
Publications
0
Known Names

Molecular Properties

314.4
MW (Da)
2.36
ALogP
4
HBA
2
HBD
72.5
PSA (Ų)
0.91
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H22N4O2
MW 314.39
Aromatic Rings 2
Heavy Atoms 23
NP-Likeness -1.42

Activity Summary

IC50 1 meas. best 6.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Transthyretin
CHEMBL3194
IC50 6.68 6.68 210.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 23.1 mL.min-1.g-1 Homo sapiens
CL 23.1 mL.min-1.g-1 Rattus norvegicus
CL 23.1 mL.min-1.g-1 Mus musculus
CL 23.1 mL.min-1.g-1 Macaca mulatta

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Transthyretin IC50 = 210.0 nM 6.68 Binding affinity to human plasma TTR tetramer assessed as displacement of diclof... 34138572

Literature References

PubMed DOI Target Context # Activities
34138572 10.1021/acs.jmedchem.1c00099 ADMET 11
34138572 10.1021/acs.jmedchem.1c00099 Unchecked 1
34138572 10.1021/acs.jmedchem.1c00099 Transthyretin 1
34138572 10.1021/acs.jmedchem.1c00099 Retinol-binding protein 4 1
34138572 10.1021/acs.jmedchem.1c00099 No relevant target 1
34138572 10.1021/acs.jmedchem.1c00099 Cytochrome P450 2C9 1
34138572 10.1021/acs.jmedchem.1c00099 Cytochrome P450 2C19 1
34138572 10.1021/acs.jmedchem.1c00099 Cytochrome P450 2D6 1
34138572 10.1021/acs.jmedchem.1c00099 Cytochrome P450 3A4 1

Data from ChEMBL 36 via Core Engine