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Compound Detail

CHEMBL2179510

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Cc1noc(-c2ccc3c(c2)c2c(n3CCCSc3cc(F)cc(F)c3)CCCC2)n1

Basic Information

ChEMBL ID CHEMBL2179510
Phase Preclinical
Structure Type MOL
InChI Key GZGZYDZBSNEDTO-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
23
PK Parameters
13
Publications
0
Known Names

Molecular Properties

439.5
MW (Da)
6.34
ALogP
5
HBA
0
HBD
43.9
PSA (Ų)
0.26
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H23F2N3OS
MW 439.53
Aromatic Rings 4
Heavy Atoms 31
NP-Likeness -1.70

Activity Summary

IC50 2 meas. best 8.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Scavenger receptor class B member 1
CHEMBL1914272
IC50 8.82 8.82 1.5 2

Pharmacokinetic Data

Parameter Value Units Species
AUC 1184.0 ng.hr.mL-1 Rattus norvegicus
AUC 143.0 ng.hr.mL-1 Rattus norvegicus
AUC 2010.0 ng.hr.mL-1 Canis lupus familiaris
AUC 4226.0 ng.hr.mL-1 Rattus norvegicus
AUC 1746.0 ng.hr.mL-1 Canis lupus familiaris
CL 28.0 mL.min-1.kg-1 Rattus norvegicus
CL 19.0 mL.min-1.kg-1 Canis lupus familiaris
Cmax 6800.45 nM Rattus norvegicus
Cmax 1421.97 nM Canis lupus familiaris
Cmax 2172.78 nM Rattus norvegicus
Cmax 8818.51 nM Canis lupus familiaris
F 34.0 % Canis lupus familiaris
F 40.0 % Rattus norvegicus
T1/2 1.5 hr Rattus norvegicus
T1/2 4.07 hr Canis lupus familiaris
T1/2 6.01 hr Rattus norvegicus
T1/2 1.1 hr Canis lupus familiaris
T1/2 0.9833 hr Rattus norvegicus
T1/2 0.7167 hr Homo sapiens
Tmax 2.0 hr Canis lupus familiaris
Tmax 2.33 hr Rattus norvegicus
Vd 3.64 L.kg-1 Rattus norvegicus
Vd 1.8 L.kg-1 Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22784640 10.1016/j.bmcl.2012.06.038 Rattus norvegicus 17
22784640 10.1016/j.bmcl.2012.06.038 Canis familiaris 10
22784640 10.1016/j.bmcl.2012.06.038 Scavenger receptor class B member 1 4
22784640 10.1016/j.bmcl.2012.06.038 Liver microsomes 2
22784640 10.1016/j.bmcl.2012.06.038 Hepatitis C virus 1
22784640 10.1016/j.bmcl.2012.06.038 Vesicular stomatitis virus 1
22784640 10.1016/j.bmcl.2012.06.038 Bovine viral diarrhea virus 1 1
22784640 10.1016/j.bmcl.2012.06.038 Cannabinoid receptor 1 1
22784640 10.1016/j.bmcl.2012.06.038 Adenosine receptor A3 1
22784640 10.1016/j.bmcl.2012.06.038 Voltage-gated inwardly rectifying potassium channel KCNH2 1
22784640 10.1016/j.bmcl.2012.06.038 Salmonella typhimurium 1
22784640 10.1016/j.bmcl.2012.06.038 Huh-7 1
22784640 10.1016/j.bmcl.2012.06.038 No relevant target 1

Data from ChEMBL 36 via Core Engine