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Compound Detail

CHEMBL42191

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COc1ccccc1CN(C[C@@H](Cc1c[nH]c2ccccc12)NC(=O)COc1ccc(-c2csnn2)cc1)C(C)=O

Basic Information

ChEMBL ID CHEMBL42191
Phase Preclinical
Structure Type MOL
InChI Key JIYMZYDKZMRNFP-RUZDIDTESA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
2
Publications
0
Known Names

Molecular Properties

569.7
MW (Da)
4.85
ALogP
7
HBA
2
HBD
109.4
PSA (Ų)
0.22
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H31N5O4S
MW 569.69
Aromatic Rings 5
Heavy Atoms 41
NP-Likeness -1.29

Activity Summary

IC50 1 meas. best 9.01

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Substance-P receptor
CHEMBL249
IC50 9.01 9.01 1.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 47.0 % Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Substance-P receptor IC50 = 0.98 nM 9.01 In vitro inhibition of binding of [125I]Bolton-Hunter SP to Tachykinin receptor ... 11425527

Literature References

PubMed DOI Target Context # Activities
11425527 10.1016/s0960-894x(01)00250-5 Canis familiaris 2
11425527 10.1016/s0960-894x(01)00250-5 Substance-P receptor 1

Data from ChEMBL 36 via Core Engine