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Compound Detail

CHEMBL4645875

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COc1ccccc1C1CCN(C(=O)N[C@H](Cc2cc(Br)c(O)c(Br)c2)C(=O)N[C@@H](CCCCN)C(=O)N2CCN(c3ccncc3)CC2)CC1

Basic Information

ChEMBL ID CHEMBL4645875
Phase Preclinical
Structure Type MOL
InChI Key CVPWNBYUSUFFDB-AJQTZOPKSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

829.6
MW (Da)
4.78
ALogP
8
HBA
4
HBD
153.4
PSA (Ų)
0.18
QED
1
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C37H47Br2N7O5
MW 829.63
Aromatic Rings 3
Heavy Atoms 51
NP-Likeness -0.57

Activity Summary

IC50 1 meas. best 6.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Calcitonin-gene-related peptide receptor, CALCRL/RAMP1
CHEMBL2107838
IC50 6.6 6.6 250.0 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 = 250.0 nM 6.6 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