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Assay Detail

CHEMBL4737518

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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 by HTRF assay
ChEMBL ↗
42
Total Activities
42
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 42 7.55 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4745611 — — 1 10.00
CHEMBL4795810 — — 1 9.70
CHEMBL4786789 — — 1 9.40
CHEMBL4754949 — — 1 9.38
CHEMBL4799907 — — 1 9.22
CHEMBL4764326 — — 1 9.00
CHEMBL4797641 — — 1 9.00
CHEMBL4752287 — — 1 8.49
CHEMBL4793799 — — 1 8.44
CHEMBL4781560 — — 1 7.92
CHEMBL4761130 — — 1 7.85
CHEMBL4784237 — — 1 7.85
CHEMBL4743539 — — 1 7.77
CHEMBL4777259 — — 1 7.77
CHEMBL4797258 — — 1 7.75
CHEMBL4744987 — — 1 7.75
CHEMBL4779982 — — 1 7.75
CHEMBL4748931 — — 1 7.71
CHEMBL4755239 — — 1 7.64
CHEMBL4791290 — — 1 7.50
CHEMBL4788675 — — 1 7.50
CHEMBL4748601 — — 1 7.43
CHEMBL4739969 — — 1 7.37
CHEMBL4748830 — — 1 7.35
CHEMBL4781139 — — 1 7.35
CHEMBL4756139 — — 1 7.34
CHEMBL4791486 — — 1 7.27
CHEMBL4785899 — — 1 7.04
CHEMBL4747756 — — 1 6.91
CHEMBL4757578 — — 1 6.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4745611 — EC50 = 0.1 nM 10.00
CHEMBL4795810 — EC50 = 0.2 nM 9.70
CHEMBL4786789 — EC50 = 0.4 nM 9.40
CHEMBL4754949 — EC50 = 0.42 nM 9.38
CHEMBL4799907 — EC50 = 0.6 nM 9.22
CHEMBL4764326 — EC50 = 1.0 nM 9.00
CHEMBL4797641 — EC50 = 1.0 nM 9.00
CHEMBL4752287 — EC50 = 3.2 nM 8.49
CHEMBL4793799 — EC50 = 3.6 nM 8.44
CHEMBL4781560 — EC50 = 12.0 nM 7.92
CHEMBL4761130 — EC50 = 14.0 nM 7.85
CHEMBL4784237 — EC50 = 14.0 nM 7.85
CHEMBL4743539 — EC50 = 17.0 nM 7.77
CHEMBL4777259 — EC50 = 17.0 nM 7.77
CHEMBL4779982 — EC50 = 17.8 nM 7.75
CHEMBL4797258 — EC50 = 17.6 nM 7.75
CHEMBL4744987 — EC50 = 18.0 nM 7.75
CHEMBL4748931 — EC50 = 19.5 nM 7.71
CHEMBL4755239 — EC50 = 23.0 nM 7.64
CHEMBL4791290 — EC50 = 32.0 nM 7.50
CHEMBL4788675 — EC50 = 32.0 nM 7.50
CHEMBL4748601 — EC50 = 37.0 nM 7.43
CHEMBL4739969 — EC50 = 43.0 nM 7.37
CHEMBL4748830 — EC50 = 45.0 nM 7.35
CHEMBL4781139 — EC50 = 45.0 nM 7.35
CHEMBL4756139 — EC50 = 46.0 nM 7.34
CHEMBL4791486 — EC50 = 54.0 nM 7.27
CHEMBL4785899 — EC50 = 92.1 nM 7.04
CHEMBL4747756 — EC50 = 124.0 nM 6.91
CHEMBL4757578 — EC50 = 143.0 nM 6.84
CHEMBL4800116 — EC50 = 146.0 nM 6.84
CHEMBL4792874 — EC50 = 202.0 nM 6.70
CHEMBL4761424 — EC50 = 200.0 nM 6.70
CHEMBL4755289 — EC50 = 230.0 nM 6.64
CHEMBL4746080 — EC50 = 368.0 nM 6.43
CHEMBL4743958 — EC50 = 393.0 nM 6.41
CHEMBL4744303 — EC50 = 498.0 nM 6.30
CHEMBL4754697 — EC50 = 522.0 nM 6.28
CHEMBL4757890 — EC50 = 708.0 nM 6.15
CHEMBL4796713 — EC50 = 809.0 nM 6.09
CHEMBL4765167 — EC50 = 897.0 nM 6.05
CHEMBL4781482 — EC50 = 929.0 nM 6.03