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Compound Detail

CHEMBL4643006

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CC(C)c1ccc(-c2ccc(Oc3cc(C(=O)N[C@@H]4CCN(C5CCOCC5)C[C@@H]4F)ccc3CN3C[C@@H](C)CC3=O)cc2)nn1

Basic Information

ChEMBL ID CHEMBL4643006
Phase Preclinical
Structure Type MOL
InChI Key OCUJZNSQSAMOBQ-MYHCNICMSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

629.8
MW (Da)
5.75
ALogP
7
HBA
1
HBD
96.9
PSA (Ų)
0.32
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C36H44FN5O4
MW 629.78
Aromatic Rings 3
Heavy Atoms 46
NP-Likeness -0.85

Activity Summary

IC50 1 meas. best 11.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Calcitonin-gene-related peptide receptor, CALCRL/RAMP1
CHEMBL2107838
IC50 11.0 11.0 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 IC50 = 0.01 nM 11.0 Inhibition of human CLR/RAMP1 by cAMP assay 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