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Compound Detail

CHEMBL3898378

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Cc1cc(C#Cc2ccc3cc(N)ccc3n2)cc(C)c1O

Basic Information

ChEMBL ID CHEMBL3898378
Phase Preclinical
Structure Type MOL
InChI Key NWQGNIAPBHQVLG-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
12
PK Parameters
2
Publications
0
Known Names

Molecular Properties

288.4
MW (Da)
3.54
ALogP
3
HBA
2
HBD
59.1
PSA (Ų)
0.49
QED
0
Ro5 Violations
0
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H16N2O
MW 288.35
Aromatic Rings 3
Heavy Atoms 22
NP-Likeness -0.40

Activity Summary

IC50 1 meas. best 5.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Transthyretin
CHEMBL3194
IC50 5.72 5.72 1900.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 232.0 ng.hr.mL-1 Rattus norvegicus
AUC 1347.0 ng.hr.mL-1 Rattus norvegicus
AUC 226.0 ng.hr.mL-1 Rattus norvegicus
AUC 1331.0 ng.hr.mL-1 Rattus norvegicus
CL 25.08 mL.min-1.kg-1 Rattus norvegicus
Cmax 478.59 nM Rattus norvegicus
Cmax 10775.1 nM Rattus norvegicus
F 6.888 % Rattus norvegicus
T1/2 1.592 hr Rattus norvegicus
T1/2 2.71 hr Rattus norvegicus
Tmax 2.45 hr Rattus norvegicus
Tmax 0.083 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Transthyretin IC50 = 1900.0 nM 5.72 Inhibition of wild type TTR (unknown origin) assessed as inhibition of acid-medi... 27541261

Literature References

PubMed DOI Target Context # Activities
27541261 10.1016/j.ejmech.2016.08.003 ADMET 13
27541261 10.1016/j.ejmech.2016.08.003 Transthyretin 3

Data from ChEMBL 36 via Core Engine