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Compound Detail

CHEMBL296013

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CC(=O)N(Cc1ccccc1Cl)C[C@@H](Cc1c[nH]c2ccccc12)NC(=O)COc1ccc(-n2ccnc2)cc1

Basic Information

ChEMBL ID CHEMBL296013
Phase Preclinical
Structure Type MOL
InChI Key RVPQJRAPQSRRCJ-RUZDIDTESA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
2
Publications
0
Known Names

Molecular Properties

556.1
MW (Da)
5.16
ALogP
5
HBA
2
HBD
92.2
PSA (Ų)
0.24
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 C31H30ClN5O3
MW 556.07
Aromatic Rings 5
Heavy Atoms 40
NP-Likeness -1.55

Activity Summary

IC50 1 meas. best 9.19

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Substance-P receptor
CHEMBL249
IC50 9.19 9.19 0.7 1

Pharmacokinetic Data

Parameter Value Units Species
F 36.0 % Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Substance-P receptor IC50 = 0.65 nM 9.19 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