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Compound Detail

CHEMBL4635521

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O=C(N[C@@H](CC1CCNCC1)C(=O)N1CCN(c2ccncc2)CC1)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(n2c(=O)[nH]c3ncccc32)CC1

Basic Information

ChEMBL ID CHEMBL4635521
Phase Preclinical
Structure Type MOL
InChI Key VJFRMTZBLLJSOE-JSOSNVBQSA-N
1
Targets
3
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

882.7
MW (Da)
3.53
ALogP
10
HBA
5
HBD
180.8
PSA (Ų)
0.16
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C38H46Br2N10O5
MW 882.66
Aromatic Rings 4
Heavy Atoms 55
NP-Likeness -0.82

Activity Summary

Ki 3 meas. best 10.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Calcitonin-gene-related peptide receptor, CALCRL/RAMP1
CHEMBL2107838
Ki 10.4 10.4 0.0 3

Pharmacokinetic Data

Parameter Value Units Species
CL 28.0 mL.min-1.kg-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32558564 10.1021/acs.jmedchem.0c01003 Calcitonin-gene-related peptide receptor, CALCRL/RAMP1 2
32558564 10.1021/acs.jmedchem.0c01003 No relevant target 2
32558564 10.1021/acs.jmedchem.0c01003 ADMET 1

Data from ChEMBL 36 via Core Engine