Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4737528

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

Functional
Agonist activity at RXFP1 endogenously expressed in human OVCAR-5 cells assessed as increase in IBMX-induced cAMP accumulation pretreated with IBMX for 40 mins followed by compound addition and measured after 30 mins in presence of 2 % HSA by HTRF assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type OVCAR-5
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Relaxin receptor 1 (CHEMBL1293316)
Type SINGLE PROTEIN
Organism Homo sapiens

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 11 7.46 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4799907 1 8.05
CHEMBL4795810 1 7.74
CHEMBL4745611 1 7.70
CHEMBL4786789 1 7.61
CHEMBL4797641 1 7.51
CHEMBL4764326 1 7.06
CHEMBL4793799 1 6.57
CHEMBL4797258 1 -
CHEMBL4752287 1 -
CHEMBL4796713 1 -
CHEMBL4746080 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4799907 EC50 = 9.0 nM 8.05
CHEMBL4795810 EC50 = 18.4 nM 7.74
CHEMBL4745611 EC50 = 19.8 nM 7.70
CHEMBL4786789 EC50 = 24.5 nM 7.61
CHEMBL4797641 EC50 = 31.0 nM 7.51
CHEMBL4764326 EC50 = 87.0 nM 7.06
CHEMBL4793799 EC50 = 270.0 nM 6.57
CHEMBL4797258 EC50 > 3000.0 nM -
CHEMBL4752287 EC50 - -
CHEMBL4796713 EC50 > 2000.0 nM -
CHEMBL4746080 EC50 > 2000.0 nM -