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Compound Detail

CHEMBL4638635

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Cc1cccc([C@H]2CC[C@@H](C(C)(C)C#N)N2C(=O)CNC(=O)c2ccc(Cc3cc(C)n[nH]c3=O)c(C)c2)c1

Basic Information

ChEMBL ID CHEMBL4638635
Phase Preclinical
Structure Type MOL
InChI Key LHCOLCAUMRHKNE-SXOMAYOGSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

525.6
MW (Da)
4.30
ALogP
5
HBA
2
HBD
119.0
PSA (Ų)
0.48
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H35N5O3
MW 525.65
Aromatic Rings 3
Heavy Atoms 39
NP-Likeness -1.10

Activity Summary

Ki 1 meas. best 10.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Calcitonin-gene-related peptide receptor, CALCRL/RAMP1
CHEMBL2107838
Ki 10.7 10.7 0.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Calcitonin-gene-related peptide receptor, CALCRL/RAMP1 Ki = 0.02 nM 10.7 Inhibition of human CLR/RAMP1 32058712

Literature References

PubMed DOI Target Context # Activities
32058712 10.1021/acs.jmedchem.9b01810 Calcitonin-gene-related peptide receptor, CALCRL/RAMP1 1

Data from ChEMBL 36 via Core Engine