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Compound Detail

CHEMBL4634646

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CN1C(=O)[C@H](NC(=O)Nc2ccc3c(c2)CC2(CC3)NC(=O)NC2=O)N=C(c2ccccc2)c2ccccc21

Basic Information

ChEMBL ID CHEMBL4634646
Phase Preclinical
Structure Type MOL
InChI Key XEPMDWDQKPFENZ-CTLOQAHHSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

522.6
MW (Da)
2.72
ALogP
5
HBA
4
HBD
132.0
PSA (Ų)
0.39
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H26N6O4
MW 522.57
Aromatic Rings 3
Heavy Atoms 39
NP-Likeness -0.53

Activity Summary

Ki 1 meas. best 5.32

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Calcitonin-gene-related peptide receptor, CALCRL/RAMP1
CHEMBL2107838
Ki 5.32 5.32 4800.0 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 = 4800.0 nM 5.32 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