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Compound Detail

CHEMBL3895601

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CN1Cc2c(Cl)cc(Cl)cc2C(c2cccc(S(=O)(=O)NCCNC(=O)C(O)C(O)C(=O)NCCNS(=O)(=O)c3cccc(C4CN(C)Cc5c(Cl)cc(Cl)cc54)c3)c2)C1

Basic Information

ChEMBL ID CHEMBL3895601
Phase Preclinical
Structure Type MOL
InChI Key RZSSNBBQYBAWBF-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
2
PK Parameters
0
Publications
0
Known Names

Molecular Properties

942.8
MW (Da)
3.67
ALogP
10
HBA
6
HBD
197.5
PSA (Ų)
0.10
QED
2
Ro5 Violations
15
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C40H44Cl4N6O8S2
MW 942.77
Aromatic Rings 4
Heavy Atoms 60
NP-Likeness -0.50

Activity Summary

IC50 1 meas. best 6.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium/hydrogen exchanger 3
CHEMBL3879842
IC50 6.0 6.0 1000.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 4.0 ng.hr.mL-1 Rattus norvegicus
Cmax 3.712 nM Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Sodium/hydrogen exchanger 3 IC50 = 1000.0 nM 6.0 Inhibition of rat NHE-3-mediated Na+ dependent H+ antiport expressed in opossum ... -

Data from ChEMBL 36 via Core Engine