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Compound Detail

CHEMBL1076241

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CS(=O)(=O)CCNCc1ccc(-c2ccc3ncnc(Nc4ccc(OCc5cccc(F)c5)c(Cl)c4)c3c2)o1.Cc1ccc(S(=O)(=O)O)cc1

Basic Information

ChEMBL ID CHEMBL1076241
Phase Preclinical
Structure Type MOL
InChI Key OZDXXJABMOYNGY-UHFFFAOYSA-N
Parent Compound CHEMBL554
Active Moiety CHEMBL554
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
6
Publications
0
Known Names

Molecular Properties

581.1
MW (Da)
6.14
ALogP
8
HBA
2
HBD
106.3
PSA (Ų)
0.18
QED
2
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C36H34ClFN4O7S2
MW 753.27
Aromatic Rings 5
Heavy Atoms 40
NP-Likeness -1.59

Activity Summary

IC50 1 meas. best 5.19

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Bile salt export pump
CHEMBL6020
IC50 5.19 5.19 6490.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 36200.66 ng.hr.mL-1 Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Bile salt export pump IC50 = 6490.0 nM 5.19 Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as... 23956101

Literature References

PubMed DOI Target Context # Activities
23956101 10.1093/toxsci/kft176 Homo sapiens 2
23956101 10.1093/toxsci/kft176 Bile salt export pump 1
23956101 10.1093/toxsci/kft176 ATP-binding cassette sub-family C member 2 1
23956101 10.1093/toxsci/kft176 ATP-binding cassette sub-family C member 3 1
23956101 10.1093/toxsci/kft176 ATP-binding cassette sub-family C member 4 1
23956101 10.1093/toxsci/kft176 Unchecked 1

Data from ChEMBL 36 via Core Engine