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Compound Detail

CHEMBL4637301

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O=C(CN1C(=O)C2(CCOC[C@H]2F)O[C@H]1c1cccc(Cl)c1)Nc1cc2c(cn1)C[C@]1(C2)C(=O)Nc2ncccc21

Basic Information

ChEMBL ID CHEMBL4637301
Phase Preclinical
Structure Type MOL
InChI Key LREUBQQMJXJGNU-KEDVGBLZSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

578.0
MW (Da)
3.11
ALogP
7
HBA
2
HBD
122.8
PSA (Ų)
0.49
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H25ClFN5O5
MW 578.00
Aromatic Rings 3
Heavy Atoms 41
NP-Likeness -0.60

Activity Summary

Ki 1 meas. best 9.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Calcitonin-gene-related peptide receptor, CALCRL/RAMP1
CHEMBL2107838
Ki 9.82 9.82 0.1 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 = 0.15 nM 9.82 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