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Compound Detail

CHEMBL103221

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Cc1cc(C)cc(C(=O)N2CC[C@H](NCc3ccnc4ccccc34)C[C@H]2Cc2ccc(C#N)cc2)c1

Basic Information

ChEMBL ID CHEMBL103221
Phase Preclinical
Structure Type MOL
InChI Key BFUFVSBGSHVEOT-URLMMPGGSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

488.6
MW (Da)
5.73
ALogP
4
HBA
1
HBD
69.0
PSA (Ų)
0.38
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H32N4O
MW 488.64
Aromatic Rings 4
Heavy Atoms 37
NP-Likeness -1.09

Activity Summary

IC50 1 meas. best 7.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Substance-P receptor
CHEMBL249
IC50 7.68 7.68 21.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Substance-P receptor IC50 = 21.0 nM 7.68 Binding affinity against NK1 receptor by displacement of [3H]SP from bovine reti... -

Literature References

PubMed DOI Target Context # Activities
- 10.1016/S0960-894X(96)00563-X Substance-P receptor 1

Data from ChEMBL 36 via Core Engine