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Assay Detail

CHEMBL4737525

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Agonist activity at rat RXFP1 expressed in human HEK296 cells assessed as increase in IBMX-induced cAMP accumulation pretreated with IBMX for 40 mins followed by compound addition and measured after 30 mins by HTRF assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Relaxin receptor 1 (CHEMBL4739859)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Identification of Potent and Long-Acting Single-Chain Peptide Mimetics of Human Relaxin-2 for Cardiovascular Diseases.
Mallart S,Ingenito R,Bianchi E,Bresciani A,Esposito S,Gallo M,Magotti P,Monteagudo E,Orsatti L,Roversi D,Santoprete A,Tucci F,Veneziano M,Bartsch R,Boehm C,Brasseur D,Bruneau P,Corbier A,Froissant J,Gauzy-Lazo L,Gervat V,Marguet F,Menguy I,Minoletti C,Nicolas MF,Pasquier O,Poirier B,Raux A,Riva L,Janiak P,Strobel H,Duclos O,Illiano S
J Med Chem (2021) 64 : 2139 -2150
PubMed 33555858 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 8.88 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4754949 1 9.30
CHEMBL4793799 1 9.05
CHEMBL4781560 1 8.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4754949 EC50 = 0.5 nM 9.30
CHEMBL4793799 EC50 = 0.9 nM 9.05
CHEMBL4781560 EC50 = 5.3 nM 8.28