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Compound Detail

CHEMBL113841

ZANKIREN
🧪 Phase II
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🧪 Phase II
CC(C)C[C@H](O)[C@H](O)[C@H](CC1CCCCC1)NC(=O)[C@H](Cc1cscn1)NC(=O)[C@H](Cc1ccccc1)CS(=O)(=O)N1CCN(C)CC1

Basic Information

ChEMBL ID CHEMBL113841
Name ZANKIREN
Phase Phase II
Structure Type MOL
InChI Key YFDSDRDMDDGDFC-HOQQKOLYSA-N

Known Names

A-72517 Zankiren Zankirene Zankireno
2
Targets
7
Activities
1
Assay Types
9
PK Parameters
11
Publications
4
Known Names

Molecular Properties

706.0
MW (Da)
2.83
ALogP
9
HBA
4
HBD
152.2
PSA (Ų)
0.20
QED
1
Ro5 Violations
17
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Single Enantiomer
USAN Stem -kiren
USAN Year 1993

Extended Properties

Molecular Formula C35H55N5O6S2
MW 705.99
Aromatic Rings 2
Heavy Atoms 48
NP-Likeness -0.38

Activity Summary

IC50 7 meas. best 9.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Renin
CHEMBL286
IC50 9.7 8.86 0.2 6
Renin
CHEMBL2322
IC50 5.85 5.85 1400.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 3800.0 ng.hr.mL-1 Simiiformes
AUC 340.0 ng.hr.mL-1 Simiiformes
AUC 1500.0 ng.hr.mL-1 Mustela putorius furo
AUC 620.0 ng.hr.mL-1 Rattus norvegicus
Cmax 0.43 ul ml-1 -
Cmax 1.15 ul ml-1 -
F 5.1 % Simiiformes
F 82.0 % Mustela putorius furo
F 23.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
8474102 10.1021/jm00056a006 ADMET 8
8474102 10.1021/jm00056a006 Renin 5
8474102 10.1021/jm00056a006 Rattus norvegicus 4
10669559 10.1021/jm990412m ADMET 3
8474102 10.1021/jm00056a006 No relevant target 2
8474102 10.1021/jm00056a006 Mustela putorius furo 2
10669559 10.1021/jm990412m Canis familiaris 1
10669559 10.1021/jm990412m Rattus norvegicus 1
10669559 10.1021/jm990412m Mustela putorius furo 1
10669559 10.1021/jm990412m Renin 1
19358611 10.1021/jm900022f Renin 1

Data from ChEMBL 36 via Core Engine