Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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 Assay
Type

 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
CHEMBL5081158 217216 None 0 Human Functional pEC50 = 8.9 8.9 -2 2
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None CCc1cc(OC)cc2c(/C=N/NC(=N)NCCc3ccc(C#N)cc3)c[nH]c12 10.1021/acs.jmedchem.1c01081
CHEMBL5094669 217997 None 0 Human Functional pEC50 = 8.9 8.9 -1 2
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None CCc1cc(C#N)cc2c(/C=N/NC(=N)NCCc3cccnc3)c[nH]c12 10.1021/acs.jmedchem.1c01081
CHEMBL5081158 217216 None 0 Human Functional pEC50 = 8.0 8.0 -2 2
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as beta arrestin-2 recruitment measured after 4 hrs by beta-galactosidase based beta arrestin2 recruitment assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as beta arrestin-2 recruitment measured after 4 hrs by beta-galactosidase based beta arrestin2 recruitment assay
ChEMBL None None None CCc1cc(OC)cc2c(/C=N/NC(=N)NCCc3ccc(C#N)cc3)c[nH]c12 10.1021/acs.jmedchem.1c01081
CHEMBL5077251 216977 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None COc1cc(C)c2[nH]cc(/C=N/NC(=N)NCCc3cccnc3)c2c1 10.1021/acs.jmedchem.1c01081
155519131 170460 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human RXFP3 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assayAgonist activity at human RXFP3 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assay
ChEMBL 2542 70 40 31 -8.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@](C)(NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CNC(C)=O)C(C)C)CCC/C=C/CCC[C@@](C)(C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)[C@@H](C)O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/acs.jmedchem.6b00265
CHEMBL4447532 170460 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human RXFP3 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assayAgonist activity at human RXFP3 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assay
ChEMBL 2542 70 40 31 -8.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@](C)(NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CNC(C)=O)C(C)C)CCC/C=C/CCC[C@@](C)(C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)[C@@H](C)O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/acs.jmedchem.6b00265
16214672 173964 None 0 Human Functional pEC50 = 5.9 5.9 1 2
Agonist activity at human RXFP3 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assayAgonist activity at human RXFP3 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assay
ChEMBL 3041 95 49 39 -10.9 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CS)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H](N)CCCNC(=N)N)C(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CS)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)O)[C@@H](C)CC)C(C)C 10.1021/acs.jmedchem.6b00265
CHEMBL4539255 173964 None 0 Human Functional pEC50 = 5.9 5.9 1 2
Agonist activity at human RXFP3 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assayAgonist activity at human RXFP3 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assay
ChEMBL 3041 95 49 39 -10.9 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CS)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H](N)CCCNC(=N)N)C(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CS)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)O)[C@@H](C)CC)C(C)C 10.1021/acs.jmedchem.6b00265
138319674 173287 None 7 Human Functional pEC50 = 6.9 6.9 -17 2
Agonist activity at human RXFP3 expressed in CHOK1 cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 3 hrs by scintillation counting methodAgonist activity at human RXFP3 expressed in CHOK1 cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 3 hrs by scintillation counting method
ChEMBL 383 6 5 3 3.8 CCc1cc(O)cc2c(/C=N/NC(=N)NCCc3ccc(Cl)cc3)c[nH]c12 10.1016/j.bmcl.2019.02.013
CHEMBL4522365 173287 None 7 Human Functional pEC50 = 6.9 6.9 -17 2
Agonist activity at human RXFP3 expressed in CHOK1 cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 3 hrs by scintillation counting methodAgonist activity at human RXFP3 expressed in CHOK1 cell membranes assessed as stimulation of [35S]-GTPgammaS binding after 3 hrs by scintillation counting method
ChEMBL 383 6 5 3 3.8 CCc1cc(O)cc2c(/C=N/NC(=N)NCCc3ccc(Cl)cc3)c[nH]c12 10.1016/j.bmcl.2019.02.013
11906 965 None 7 Human Functional pEC50 = 7.9 7.9 -1 2
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as beta arrestin-2 recruitment measured after 4 hrs by beta-galactosidase based beta arrestin2 recruitment assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as beta arrestin-2 recruitment measured after 4 hrs by beta-galactosidase based beta arrestin2 recruitment assay
ChEMBL 402 6 4 5 2.8 C(#N)c1cc2c(c[nH]c2c(c1)C)/C=N/NC(=N)NCCc1ccc(C(=O)OC)cc1 10.1021/acs.jmedchem.1c01081
162679544 965 None 7 Human Functional pEC50 = 7.9 7.9 -1 2
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as beta arrestin-2 recruitment measured after 4 hrs by beta-galactosidase based beta arrestin2 recruitment assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as beta arrestin-2 recruitment measured after 4 hrs by beta-galactosidase based beta arrestin2 recruitment assay
ChEMBL 402 6 4 5 2.8 C(#N)c1cc2c(c[nH]c2c(c1)C)/C=N/NC(=N)NCCc1ccc(C(=O)OC)cc1 10.1021/acs.jmedchem.1c01081
CHEMBL5089949 965 None 7 Human Functional pEC50 = 7.9 7.9 -1 2
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as beta arrestin-2 recruitment measured after 4 hrs by beta-galactosidase based beta arrestin2 recruitment assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as beta arrestin-2 recruitment measured after 4 hrs by beta-galactosidase based beta arrestin2 recruitment assay
ChEMBL 402 6 4 5 2.8 C(#N)c1cc2c(c[nH]c2c(c1)C)/C=N/NC(=N)NCCc1ccc(C(=O)OC)cc1 10.1021/acs.jmedchem.1c01081
CHEMBL5075621 216875 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None COc1cc(C)c2[nH]cc(/C=N/NC(=N)NCCc3cccc(Cl)c3)c2c1 10.1021/acs.jmedchem.1c01081
162661752 181951 None 0 Human Functional pEC50 = 7.9 7.9 21 2
Agonist activity at RXFP3 (unknown origin) stably expressed in CHO-K1 cells co-transfected with pCRE assessed as inhibition of forskolin-induced cAMP accumulation measured after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at RXFP3 (unknown origin) stably expressed in CHO-K1 cells co-transfected with pCRE assessed as inhibition of forskolin-induced cAMP accumulation measured after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 4636 96 71 63 -15.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)N[C@H](CO)Cc2c[nH]c3ccccc23)C(C)C)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC1=O 10.1021/acsmedchemlett.0c00456
CHEMBL4778498 181951 None 0 Human Functional pEC50 = 7.9 7.9 21 2
Agonist activity at RXFP3 (unknown origin) stably expressed in CHO-K1 cells co-transfected with pCRE assessed as inhibition of forskolin-induced cAMP accumulation measured after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at RXFP3 (unknown origin) stably expressed in CHO-K1 cells co-transfected with pCRE assessed as inhibition of forskolin-induced cAMP accumulation measured after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 4636 96 71 63 -15.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)N[C@H](CO)Cc2c[nH]c3ccccc23)C(C)C)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC1=O 10.1021/acsmedchemlett.0c00456
CHEMBL5094670 217998 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None COc1cc(C)c2[nH]cc(/C=N/NC(=N)NCCc3ccc(C#N)cc3)c2c1 10.1021/acs.jmedchem.1c01081
CHEMBL5078386 217042 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None COc1cc(C)c2[nH]cc(/C=N/NC(=N)NCCc3ccc([N+](=O)[O-])cc3)c2c1 10.1021/acs.jmedchem.1c01081
155552669 174249 None 0 Human Functional pEC50 = 5.9 5.9 -3 2
Agonist activity at human RXFP3 expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation preincubated for 30 mins followed by forskolin-stimulation and measured after 30 mins by HTRF assayAgonist activity at human RXFP3 expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation preincubated for 30 mins followed by forskolin-stimulation and measured after 30 mins by HTRF assay
ChEMBL 383 6 4 3 3.8 COc1cc(C)c2[nH]cc(/C=N/NC(=N)NCCc3ccc(Cl)cc3)c2c1 10.1016/j.bmcl.2019.02.013
CHEMBL4546426 174249 None 0 Human Functional pEC50 = 5.9 5.9 -3 2
Agonist activity at human RXFP3 expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation preincubated for 30 mins followed by forskolin-stimulation and measured after 30 mins by HTRF assayAgonist activity at human RXFP3 expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation preincubated for 30 mins followed by forskolin-stimulation and measured after 30 mins by HTRF assay
ChEMBL 383 6 4 3 3.8 COc1cc(C)c2[nH]cc(/C=N/NC(=N)NCCc3ccc(Cl)cc3)c2c1 10.1016/j.bmcl.2019.02.013
CHEMBL5090612 217765 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None N=C(NCCc1ccc(Cl)cc1)N/N=C/c1c[nH]c2ccc(F)cc12 10.1021/acs.jmedchem.1c01081
162675340 183565 None 0 Human Functional pEC50 = 7.8 7.8 -1 2
Agonist activity at RXFP3 (unknown origin) stably expressed in CHO-K1 cells co-transfected with pCRE assessed as inhibition of forskolin-induced cAMP accumulation measured after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at RXFP3 (unknown origin) stably expressed in CHO-K1 cells co-transfected with pCRE assessed as inhibition of forskolin-induced cAMP accumulation measured after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 4649 96 71 63 -16.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C(C)C)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC1=O 10.1021/acsmedchemlett.0c00456
CHEMBL4799017 183565 None 0 Human Functional pEC50 = 7.8 7.8 -1 2
Agonist activity at RXFP3 (unknown origin) stably expressed in CHO-K1 cells co-transfected with pCRE assessed as inhibition of forskolin-induced cAMP accumulation measured after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at RXFP3 (unknown origin) stably expressed in CHO-K1 cells co-transfected with pCRE assessed as inhibition of forskolin-induced cAMP accumulation measured after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 4649 96 71 63 -16.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C(C)C)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC1=O 10.1021/acsmedchemlett.0c00456
CHEMBL5083794 217371 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None COc1cc(C)c2[nH]cc(/C=N/NC(=N)NCCCc3ccc(Cl)cc3)c2c1 10.1021/acs.jmedchem.1c01081
CHEMBL5074457 216806 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None COc1ccc2[nH]cc(/C=N/NC(=N)NCCc3ccc(Cl)cc3)c2c1 10.1021/acs.jmedchem.1c01081
138319674 173287 None 7 Human Functional pEC50 = 7.7 7.7 -17 2
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL 383 6 5 3 3.8 CCc1cc(O)cc2c(/C=N/NC(=N)NCCc3ccc(Cl)cc3)c[nH]c12 10.1021/acs.jmedchem.1c01081
CHEMBL4522365 173287 None 7 Human Functional pEC50 = 7.7 7.7 -17 2
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL 383 6 5 3 3.8 CCc1cc(O)cc2c(/C=N/NC(=N)NCCc3ccc(Cl)cc3)c[nH]c12 10.1021/acs.jmedchem.1c01081
CHEMBL5080438 217174 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None CCc1cc(OC)cc2c(/C=N/NC(=N)NCCc3ccc(Cl)cc3)c[nH]c12 10.1021/acs.jmedchem.1c01081
CHEMBL5084331 217397 None 0 Human Functional pEC50 = 8.6 8.6 -2 2
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None CCc1cc(OC)cc2c(/C=N/NC(=N)NCCc3cccnc3)c[nH]c12 10.1021/acs.jmedchem.1c01081
138319674 173287 None 7 Human Functional pEC50 = 7.7 7.7 -17 2
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as beta arrestin-2 recruitment measured after 4 hrs by beta-galactosidase based beta arrestin2 recruitment assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as beta arrestin-2 recruitment measured after 4 hrs by beta-galactosidase based beta arrestin2 recruitment assay
ChEMBL 383 6 5 3 3.8 CCc1cc(O)cc2c(/C=N/NC(=N)NCCc3ccc(Cl)cc3)c[nH]c12 10.1021/acs.jmedchem.1c01081
CHEMBL4522365 173287 None 7 Human Functional pEC50 = 7.7 7.7 -17 2
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as beta arrestin-2 recruitment measured after 4 hrs by beta-galactosidase based beta arrestin2 recruitment assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as beta arrestin-2 recruitment measured after 4 hrs by beta-galactosidase based beta arrestin2 recruitment assay
ChEMBL 383 6 5 3 3.8 CCc1cc(O)cc2c(/C=N/NC(=N)NCCc3ccc(Cl)cc3)c[nH]c12 10.1021/acs.jmedchem.1c01081
CHEMBL5089400 217697 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None COc1cc(C)c2[nH]cc(/C=N/NC(=N)NCCc3ccccc3)c2c1 10.1021/acs.jmedchem.1c01081
CHEMBL5093542 217921 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None COc1cc(C)c2[nH]cc(/C=N/NC(=N)NCCc3ccc(C)cc3)c2c1 10.1021/acs.jmedchem.1c01081
CHEMBL5077014 216961 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None N#Cc1ccc2[nH]cc(/C=N/NC(=N)NCCc3ccc(Cl)cc3)c2c1 10.1021/acs.jmedchem.1c01081
155566939 175995 None 0 Human Functional pEC50 = 5.6 5.6 -15 2
Agonist activity at human RXFP3 expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation preincubated for 30 mins followed by forskolin-stimulation and measured after 30 mins by HTRF assayAgonist activity at human RXFP3 expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation preincubated for 30 mins followed by forskolin-stimulation and measured after 30 mins by HTRF assay
ChEMBL 417 6 4 3 4.5 COc1cc(C)c2[nH]cc(/C=N/NC(=N)NCCc3ccc(Cl)c(Cl)c3)c2c1 10.1016/j.bmcl.2019.02.013
CHEMBL4586446 175995 None 0 Human Functional pEC50 = 5.6 5.6 -15 2
Agonist activity at human RXFP3 expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation preincubated for 30 mins followed by forskolin-stimulation and measured after 30 mins by HTRF assayAgonist activity at human RXFP3 expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation preincubated for 30 mins followed by forskolin-stimulation and measured after 30 mins by HTRF assay
ChEMBL 417 6 4 3 4.5 COc1cc(C)c2[nH]cc(/C=N/NC(=N)NCCc3ccc(Cl)c(Cl)c3)c2c1 10.1016/j.bmcl.2019.02.013
155566939 175995 None 0 Human Functional pEC50 = 5.6 5.6 -15 2
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as beta arrestin-2 recruitment measured after 4 hrs by beta-galactosidase based beta arrestin2 recruitment assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as beta arrestin-2 recruitment measured after 4 hrs by beta-galactosidase based beta arrestin2 recruitment assay
ChEMBL 417 6 4 3 4.5 COc1cc(C)c2[nH]cc(/C=N/NC(=N)NCCc3ccc(Cl)c(Cl)c3)c2c1 10.1021/acs.jmedchem.1c01081
CHEMBL4586446 175995 None 0 Human Functional pEC50 = 5.6 5.6 -15 2
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as beta arrestin-2 recruitment measured after 4 hrs by beta-galactosidase based beta arrestin2 recruitment assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as beta arrestin-2 recruitment measured after 4 hrs by beta-galactosidase based beta arrestin2 recruitment assay
ChEMBL 417 6 4 3 4.5 COc1cc(C)c2[nH]cc(/C=N/NC(=N)NCCc3ccc(Cl)c(Cl)c3)c2c1 10.1021/acs.jmedchem.1c01081
CHEMBL5072912 216777 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None COc1cc(C)c2[nH]cc(/C=N/NC(=N)NCCc3ccncc3)c2c1 10.1021/acs.jmedchem.1c01081
CHEMBL5090147 217734 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None N=C(NCCc1ccc(Cl)cc1)N/N=C/c1c[nH]c2c(F)cccc12 10.1021/acs.jmedchem.1c01081
CHEMBL5089792 217718 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None N=C(NCCc1ccc(Cl)cc1)N/N=C/c1c[nH]c2ccc(Cl)cc12 10.1021/acs.jmedchem.1c01081
11906 965 None 7 Human Functional pEC50 = 8.5 8.5 -1 2
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL 402 6 4 5 2.8 C(#N)c1cc2c(c[nH]c2c(c1)C)/C=N/NC(=N)NCCc1ccc(C(=O)OC)cc1 10.1021/acs.jmedchem.1c01081
162679544 965 None 7 Human Functional pEC50 = 8.5 8.5 -1 2
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL 402 6 4 5 2.8 C(#N)c1cc2c(c[nH]c2c(c1)C)/C=N/NC(=N)NCCc1ccc(C(=O)OC)cc1 10.1021/acs.jmedchem.1c01081
CHEMBL5089949 965 None 7 Human Functional pEC50 = 8.5 8.5 -1 2
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL 402 6 4 5 2.8 C(#N)c1cc2c(c[nH]c2c(c1)C)/C=N/NC(=N)NCCc1ccc(C(=O)OC)cc1 10.1021/acs.jmedchem.1c01081
155554720 174708 None 0 Human Functional pEC50 = 8.5 8.5 177 2
Agonist activity at human RXFP3 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assayAgonist activity at human RXFP3 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assay
ChEMBL 2117 55 33 26 -6.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@](C)(NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(C)=O)CCC/C=C/CCC[C@@](C)(C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)[C@@H](C)O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/acs.jmedchem.6b00265
CHEMBL4557279 174708 None 0 Human Functional pEC50 = 8.5 8.5 177 2
Agonist activity at human RXFP3 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assayAgonist activity at human RXFP3 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assay
ChEMBL 2117 55 33 26 -6.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@](C)(NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(C)=O)CCC/C=C/CCC[C@@](C)(C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)[C@@H](C)O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/acs.jmedchem.6b00265
155549840 173999 None 0 Human Functional pEC50 = 8.5 8.5 34 2
Agonist activity at human RXFP3 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assayAgonist activity at human RXFP3 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assay
ChEMBL 2344 64 38 29 -7.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@](C)(NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CCCNC(=N)N)CCC/C=C/CCC[C@@](C)(C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)[C@@H](C)O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/acs.jmedchem.6b00265
CHEMBL4540069 173999 None 0 Human Functional pEC50 = 8.5 8.5 34 2
Agonist activity at human RXFP3 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assayAgonist activity at human RXFP3 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assay
ChEMBL 2344 64 38 29 -7.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@](C)(NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CCCNC(=N)N)CCC/C=C/CCC[C@@](C)(C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)[C@@H](C)O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/acs.jmedchem.6b00265
155566939 175995 None 0 Human Functional pEC50 = 6.5 6.5 -15 2
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL 417 6 4 3 4.5 COc1cc(C)c2[nH]cc(/C=N/NC(=N)NCCc3ccc(Cl)c(Cl)c3)c2c1 10.1021/acs.jmedchem.1c01081
CHEMBL4586446 175995 None 0 Human Functional pEC50 = 6.5 6.5 -15 2
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL 417 6 4 3 4.5 COc1cc(C)c2[nH]cc(/C=N/NC(=N)NCCc3ccc(Cl)c(Cl)c3)c2c1 10.1021/acs.jmedchem.1c01081
CHEMBL5080373 217168 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None COC(=O)c1ccc2[nH]cc(/C=N/NC(=N)NCCc3ccc(Cl)cc3)c2c1 10.1021/acs.jmedchem.1c01081
CHEMBL5077950 217012 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None COc1cc(C)c2[nH]cc(/C=N/NC(=N)Nc3ccc(Cl)cc3)c2c1 10.1021/acs.jmedchem.1c01081
CHEMBL5094362 217979 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None N=C(NCCc1ccc(Cl)cc1)N/N=C/c1c[nH]c2ccc([N+](=O)[O-])cc12 10.1021/acs.jmedchem.1c01081
CHEMBL5084549 217412 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None N=C(NCCc1ccc(Cl)cc1)N/N=C/c1c[nH]c2cccc(F)c12 10.1021/acs.jmedchem.1c01081
CHEMBL5084224 217393 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None N=C(NCCc1ccc(Cl)cc1)N/N=C/c1c[nH]c2cc(F)ccc12 10.1021/acs.jmedchem.1c01081
CHEMBL5093979 217952 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None COc1cc(C)c2[nH]cc(/C=N/NC(=N)NCc3ccc(Cl)cc3)c2c1 10.1021/acs.jmedchem.1c01081
162664973 182170 None 0 Human Functional pEC50 = 8.4 8.4 1 2
Agonist activity at RXFP3 (unknown origin) stably expressed in CHO-K1 cells co-transfected with pCRE assessed as inhibition of forskolin-induced cAMP accumulation measured after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at RXFP3 (unknown origin) stably expressed in CHO-K1 cells co-transfected with pCRE assessed as inhibition of forskolin-induced cAMP accumulation measured after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 4778 100 72 66 -16.9 CC[C@H](C)[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)OC[C@H](NC(C)=O)C(N)=O)C(C)C)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC1=O 10.1021/acsmedchemlett.0c00456
CHEMBL4781389 182170 None 0 Human Functional pEC50 = 8.4 8.4 1 2
Agonist activity at RXFP3 (unknown origin) stably expressed in CHO-K1 cells co-transfected with pCRE assessed as inhibition of forskolin-induced cAMP accumulation measured after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at RXFP3 (unknown origin) stably expressed in CHO-K1 cells co-transfected with pCRE assessed as inhibition of forskolin-induced cAMP accumulation measured after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 4778 100 72 66 -16.9 CC[C@H](C)[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)OC[C@H](NC(C)=O)C(N)=O)C(C)C)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC1=O 10.1021/acsmedchemlett.0c00456
155511404 169656 None 0 Human Functional pEC50 = 8.4 8.4 42 2
Agonist activity at human RXFP3 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assayAgonist activity at human RXFP3 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assay
ChEMBL 2075 54 33 26 -6.7 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@](C)(NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](N)CO)CCC/C=C/CCC[C@@](C)(C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)[C@@H](C)O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/acs.jmedchem.6b00265
CHEMBL4435599 169656 None 0 Human Functional pEC50 = 8.4 8.4 42 2
Agonist activity at human RXFP3 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assayAgonist activity at human RXFP3 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assay
ChEMBL 2075 54 33 26 -6.7 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@](C)(NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](N)CO)CCC/C=C/CCC[C@@](C)(C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)[C@@H](C)O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/acs.jmedchem.6b00265
155538336 172489 None 0 Human Functional pEC50 = 8.4 8.4 70 2
Agonist activity at human RXFP3 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assayAgonist activity at human RXFP3 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assay
ChEMBL 2500 69 40 31 -8.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@](C)(NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CN)C(C)C)CCC/C=C/CCC[C@@](C)(C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)[C@@H](C)O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/acs.jmedchem.6b00265
CHEMBL4476408 172489 None 0 Human Functional pEC50 = 8.4 8.4 70 2
Agonist activity at human RXFP3 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assayAgonist activity at human RXFP3 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assay
ChEMBL 2500 69 40 31 -8.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@](C)(NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CN)C(C)C)CCC/C=C/CCC[C@@](C)(C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)[C@@H](C)O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/acs.jmedchem.6b00265
155563106 175403 None 0 Human Functional pEC50 = 5.3 5.3 1 2
Agonist activity at human RXFP3 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assayAgonist activity at human RXFP3 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assay
ChEMBL 2124 70 35 28 -9.2 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)O)[C@@H](C)CC)C(C)C 10.1021/acs.jmedchem.6b00265
CHEMBL4573196 175403 None 0 Human Functional pEC50 = 5.3 5.3 1 2
Agonist activity at human RXFP3 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assayAgonist activity at human RXFP3 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assay
ChEMBL 2124 70 35 28 -9.2 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)O)[C@@H](C)CC)C(C)C 10.1021/acs.jmedchem.6b00265
CHEMBL5080062 217151 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None COc1ccc2c(/C=N/NC(=N)NCCc3ccc(Cl)cc3)c[nH]c2c1 10.1021/acs.jmedchem.1c01081
CHEMBL5080322 217167 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None COc1cccc2c(/C=N/NC(=N)NCCc3ccc(Cl)cc3)c[nH]c12 10.1021/acs.jmedchem.1c01081
155513302 169850 None 0 Human Functional pEC50 = 8.3 8.3 22 2
Agonist activity at human RXFP3 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assayAgonist activity at human RXFP3 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assay
ChEMBL 2386 65 38 29 -7.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@](C)(NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CCC/C=C/CCC[C@@](C)(C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)[C@@H](C)O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/acs.jmedchem.6b00265
CHEMBL4438620 169850 None 0 Human Functional pEC50 = 8.3 8.3 22 2
Agonist activity at human RXFP3 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assayAgonist activity at human RXFP3 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assay
ChEMBL 2386 65 38 29 -7.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@](C)(NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CCC/C=C/CCC[C@@](C)(C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)[C@@H](C)O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/acs.jmedchem.6b00265
CHEMBL5083969 217381 None 0 Human Functional pEC50 = 8.3 8.3 -1 2
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None CCc1cc(OC)cc2c(/C=N/NC(=N)NCCc3ccc(F)cc3)c[nH]c12 10.1021/acs.jmedchem.1c01081
CHEMBL5078678 217066 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None COc1cc(C)c2[nH]cc(/C=N/NC(=N)NCCc3ccc(F)cc3)c2c1 10.1021/acs.jmedchem.1c01081
CHEMBL5091447 217798 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None N=C(NCCc1ccc(Cl)cc1)N/N=C/c1c[nH]c2ccc(Br)cc12 10.1021/acs.jmedchem.1c01081
CHEMBL5094396 217980 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None COc1cc(C)c2[nH]cc(/C=N/NC(=N)NCCc3ccsc3)c2c1 10.1021/acs.jmedchem.1c01081
CHEMBL5076246 216910 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None COc1ccc(CCNC(=N)N/N=C/c2c[nH]c3c(C)cc(OC)cc23)cc1 10.1021/acs.jmedchem.1c01081
162659068 181364 None 0 Human Functional pEC50 = 8.2 8.2 1 2
Agonist activity at RXFP3 (unknown origin) stably expressed in CHO-K1 cells co-transfected with pCRE assessed as inhibition of forskolin-induced cAMP accumulation measured after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at RXFP3 (unknown origin) stably expressed in CHO-K1 cells co-transfected with pCRE assessed as inhibition of forskolin-induced cAMP accumulation measured after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 4650 96 71 63 -15.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)C(C)C)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC1=O 10.1021/acsmedchemlett.0c00456
CHEMBL4761849 181364 None 0 Human Functional pEC50 = 8.2 8.2 1 2
Agonist activity at RXFP3 (unknown origin) stably expressed in CHO-K1 cells co-transfected with pCRE assessed as inhibition of forskolin-induced cAMP accumulation measured after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at RXFP3 (unknown origin) stably expressed in CHO-K1 cells co-transfected with pCRE assessed as inhibition of forskolin-induced cAMP accumulation measured after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 4650 96 71 63 -15.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)C(C)C)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC1=O 10.1021/acsmedchemlett.0c00456
162661135 181613 None 0 Human Functional pEC50 = 8.2 8.2 3 2
Agonist activity at RXFP3 (unknown origin) stably expressed in CHO-K1 cells co-transfected with pCRE assessed as inhibition of forskolin-induced cAMP accumulation measured after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at RXFP3 (unknown origin) stably expressed in CHO-K1 cells co-transfected with pCRE assessed as inhibition of forskolin-induced cAMP accumulation measured after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 4679 97 71 64 -15.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)N[C@H](COC(N)=O)Cc2c[nH]c3ccccc23)C(C)C)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC1=O 10.1021/acsmedchemlett.0c00456
CHEMBL4764969 181613 None 0 Human Functional pEC50 = 8.2 8.2 3 2
Agonist activity at RXFP3 (unknown origin) stably expressed in CHO-K1 cells co-transfected with pCRE assessed as inhibition of forskolin-induced cAMP accumulation measured after 6 hrs by beta-galactosidase reporter gene assayAgonist activity at RXFP3 (unknown origin) stably expressed in CHO-K1 cells co-transfected with pCRE assessed as inhibition of forskolin-induced cAMP accumulation measured after 6 hrs by beta-galactosidase reporter gene assay
ChEMBL 4679 97 71 64 -15.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)N[C@H](COC(N)=O)Cc2c[nH]c3ccccc23)C(C)C)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC1=O 10.1021/acsmedchemlett.0c00456
CHEMBL5082989 217325 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None Cc1cccc2c(/C=N/NC(=N)NCCc3ccc(Cl)cc3)c[nH]c12 10.1021/acs.jmedchem.1c01081
CHEMBL5075697 216879 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None COc1cc(C)c2[nH]cc(/C=N/NC(=N)NCCc3ccc(I)cc3)c2c1 10.1021/acs.jmedchem.1c01081
CHEMBL5084431 217405 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None COc1cc(C)c2[nH]cc(/C=N/NC(=N)NCCc3ccc(Br)cc3)c2c1 10.1021/acs.jmedchem.1c01081
CHEMBL5084645 217417 None 4 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None N=C(NCCc1ccc(Cl)cc1)N/N=C/c1c[nH]c2ccccc12 10.1021/acs.jmedchem.1c01081
CHEMBL5072593 216772 None 0 Human Functional pEC50 = 8.1 8.1 -2 2
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None COC(=O)c1ccc(CCNC(=N)N/N=C/c2c[nH]c3c(C)cc(OC)cc23)cc1 10.1021/acs.jmedchem.1c01081
CHEMBL5078074 217021 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None COc1cc(C)c2[nH]cc(/C=N/NC(=N)NCCc3cccs3)c2c1 10.1021/acs.jmedchem.1c01081
155552669 174249 None 0 Human Functional pEC50 = 7.1 7.1 -3 2
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL 383 6 4 3 3.8 COc1cc(C)c2[nH]cc(/C=N/NC(=N)NCCc3ccc(Cl)cc3)c2c1 10.1021/acs.jmedchem.1c01081
CHEMBL4546426 174249 None 0 Human Functional pEC50 = 7.1 7.1 -3 2
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL 383 6 4 3 3.8 COc1cc(C)c2[nH]cc(/C=N/NC(=N)NCCc3ccc(Cl)cc3)c2c1 10.1021/acs.jmedchem.1c01081
CHEMBL5077878 217007 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None Cc1ccc2c(/C=N/NC(=N)NCCc3ccc(Cl)cc3)c[nH]c2c1 10.1021/acs.jmedchem.1c01081
CHEMBL5087582 217599 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None COc1ccc2[nH]cc(/C(C)=N/NC(=N)NCCc3ccc(Cl)cc3)c2c1 10.1021/acs.jmedchem.1c01081
CHEMBL5073543 216785 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None COc1cc(C)c2[nH]cc(/C=N/NC(=N)NCCc3ccccc3Cl)c2c1 10.1021/acs.jmedchem.1c01081
155534581 172053 None 0 Human Functional pEC50 = 6.1 6.1 -199 2
Agonist activity at human RXFP3 expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation preincubated for 30 mins followed by forskolin-stimulation and measured after 30 mins by HTRF assayAgonist activity at human RXFP3 expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation preincubated for 30 mins followed by forskolin-stimulation and measured after 30 mins by HTRF assay
ChEMBL 403 5 5 3 4.2 Cc1cc(O)cc2c(/C=N/NC(=N)NCCc3ccc(Cl)c(Cl)c3)c[nH]c12 10.1016/j.bmcl.2019.02.013
CHEMBL4470544 172053 None 0 Human Functional pEC50 = 6.1 6.1 -199 2
Agonist activity at human RXFP3 expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation preincubated for 30 mins followed by forskolin-stimulation and measured after 30 mins by HTRF assayAgonist activity at human RXFP3 expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation preincubated for 30 mins followed by forskolin-stimulation and measured after 30 mins by HTRF assay
ChEMBL 403 5 5 3 4.2 Cc1cc(O)cc2c(/C=N/NC(=N)NCCc3ccc(Cl)c(Cl)c3)c[nH]c12 10.1016/j.bmcl.2019.02.013
138319674 173287 None 7 Human Functional pEC50 = 7.1 7.1 -17 2
Agonist activity at human RXFP3 expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation preincubated for 30 mins followed by forskolin-stimulation and measured after 30 mins by HTRF assayAgonist activity at human RXFP3 expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation preincubated for 30 mins followed by forskolin-stimulation and measured after 30 mins by HTRF assay
ChEMBL 383 6 5 3 3.8 CCc1cc(O)cc2c(/C=N/NC(=N)NCCc3ccc(Cl)cc3)c[nH]c12 10.1016/j.bmcl.2019.02.013
CHEMBL4522365 173287 None 7 Human Functional pEC50 = 7.1 7.1 -17 2
Agonist activity at human RXFP3 expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation preincubated for 30 mins followed by forskolin-stimulation and measured after 30 mins by HTRF assayAgonist activity at human RXFP3 expressed in CHOK1 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation preincubated for 30 mins followed by forskolin-stimulation and measured after 30 mins by HTRF assay
ChEMBL 383 6 5 3 3.8 CCc1cc(O)cc2c(/C=N/NC(=N)NCCc3ccc(Cl)cc3)c[nH]c12 10.1016/j.bmcl.2019.02.013
CHEMBL5078324 217038 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None Cc1cc(C#N)cc2c(/C=N/NC(=N)NCCc3ccc(Cl)cc3)c[nH]c12 10.1021/acs.jmedchem.1c01081
CHEMBL5089682 217711 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None COc1cc(C)c2[nH]cc(/C=N/NC(=N)NCCc3ccccn3)c2c1 10.1021/acs.jmedchem.1c01081
155556159 174611 None 0 Human Functional pEC50 = 5.1 5.1 -3 2
Agonist activity at human RXFP3 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assayAgonist activity at human RXFP3 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assay
ChEMBL 2067 66 34 27 -9.3 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)O)[C@@H](C)CC)C(C)C 10.1021/acs.jmedchem.6b00265
CHEMBL4555053 174611 None 0 Human Functional pEC50 = 5.1 5.1 -3 2
Agonist activity at human RXFP3 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assayAgonist activity at human RXFP3 receptor expressed in CHOK1 cells cotransfected with beta-galactosidase assessed as inhibition of forskolin-stimulated cAMP by beta-galactosidase reporter gene assay
ChEMBL 2067 66 34 27 -9.3 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(C)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)O)[C@@H](C)CC)C(C)C 10.1021/acs.jmedchem.6b00265
CHEMBL5082272 217286 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assayAgonist activity at human RXFP3 expressed in human CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 1.5 hrs by TR-FRET assay
ChEMBL None None None COc1cc(C)c2[nH]cc(/C=N/NC(=N)NCCc3ccc(N(C)C)cc3)c2c1 10.1021/acs.jmedchem.1c01081
CHEMBL2030702 211616 None 0 Human Functional pIC50 = 7.9 7.9 -3 2
Agonist activity at RXFP3 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs by beta galactosidase reporter gene assayAgonist activity at RXFP3 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs by beta galactosidase reporter gene assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](N)CSSC[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)O)CSSC[C@@H](C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](C(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm201505p
12120 3336 None 18 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as inhibition of relaxin-3 stimulated ERK1/2 phosphorylation preincubated for 15 mins followed by relaxin-3 addition for 5 minsAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as inhibition of relaxin-3 stimulated ERK1/2 phosphorylation preincubated for 15 mins followed by relaxin-3 addition for 5 mins
ChEMBL 462 6 1 6 4.6 O=C1CC(C(=O)Nc2ccc(c3nc(c4ccc(Cl)cc4)no3)cc2)CN1Cc1ccco1 10.1021/acs.jmedchem.2c00508
164886639 3336 None 18 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as inhibition of relaxin-3 stimulated ERK1/2 phosphorylation preincubated for 15 mins followed by relaxin-3 addition for 5 minsAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as inhibition of relaxin-3 stimulated ERK1/2 phosphorylation preincubated for 15 mins followed by relaxin-3 addition for 5 mins
ChEMBL 462 6 1 6 4.6 O=C1CC(C(=O)Nc2ccc(c3nc(c4ccc(Cl)cc4)no3)cc2)CN1Cc1ccco1 10.1021/acs.jmedchem.2c00508
CHEMBL5207128 3336 None 18 Human Functional pIC50 = 4.9 4.9 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as inhibition of relaxin-3 stimulated ERK1/2 phosphorylation preincubated for 15 mins followed by relaxin-3 addition for 5 minsAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as inhibition of relaxin-3 stimulated ERK1/2 phosphorylation preincubated for 15 mins followed by relaxin-3 addition for 5 mins
ChEMBL 462 6 1 6 4.6 O=C1CC(C(=O)Nc2ccc(c3nc(c4ccc(Cl)cc4)no3)cc2)CN1Cc1ccco1 10.1021/acs.jmedchem.2c00508
165117348 189998 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assay
ChEMBL 507 6 1 6 4.8 O=C(Nc1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)no2)cc1)C1CC(=O)N(Cc2cccnc2)C1 10.1021/acs.jmedchem.2c00508
CHEMBL5169478 189998 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assay
ChEMBL 507 6 1 6 4.8 O=C(Nc1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)no2)cc1)C1CC(=O)N(Cc2cccnc2)C1 10.1021/acs.jmedchem.2c00508
165117342 190508 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assay
ChEMBL 453 6 1 6 4.1 Cc1ccc(-c2noc(-c3ccc(NC(=O)C4CC(=O)N(Cc5cccnc5)C4)cc3)n2)cc1 10.1021/acs.jmedchem.2c00508
CHEMBL5177617 190508 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assay
ChEMBL 453 6 1 6 4.1 Cc1ccc(-c2noc(-c3ccc(NC(=O)C4CC(=O)N(Cc5cccnc5)C4)cc3)n2)cc1 10.1021/acs.jmedchem.2c00508
165117364 192466 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assay
ChEMBL 439 6 1 6 3.8 O=C(Nc1ccc(-c2nc(-c3ccccc3)no2)cc1)C1CC(=O)N(Cc2cccnc2)C1 10.1021/acs.jmedchem.2c00508
CHEMBL5207177 192466 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assay
ChEMBL 439 6 1 6 3.8 O=C(Nc1ccc(-c2nc(-c3ccccc3)no2)cc1)C1CC(=O)N(Cc2cccnc2)C1 10.1021/acs.jmedchem.2c00508
165117337 190961 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assay
ChEMBL 517 6 1 6 4.5 O=C(Nc1ccc(-c2nc(-c3ccc(Br)cc3)no2)cc1)C1CC(=O)N(Cc2cccnc2)C1 10.1021/acs.jmedchem.2c00508
CHEMBL5184518 190961 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assay
ChEMBL 517 6 1 6 4.5 O=C(Nc1ccc(-c2nc(-c3ccc(Br)cc3)no2)cc1)C1CC(=O)N(Cc2cccnc2)C1 10.1021/acs.jmedchem.2c00508
165117366 191335 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding incubated for 1 hr by [35S]GTP-gammaS binding assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding incubated for 1 hr by [35S]GTP-gammaS binding assay
ChEMBL 473 6 1 6 4.4 O=C(Nc1ccc(-c2nc(-c3ccc(Cl)cc3)no2)cc1)C1CC(=O)N(Cc2cccnc2)C1 10.1021/acs.jmedchem.2c00508
CHEMBL5189833 191335 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding incubated for 1 hr by [35S]GTP-gammaS binding assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding incubated for 1 hr by [35S]GTP-gammaS binding assay
ChEMBL 473 6 1 6 4.4 O=C(Nc1ccc(-c2nc(-c3ccc(Cl)cc3)no2)cc1)C1CC(=O)N(Cc2cccnc2)C1 10.1021/acs.jmedchem.2c00508
12120 3336 None 18 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assay
ChEMBL 462 6 1 6 4.6 O=C1CC(C(=O)Nc2ccc(c3nc(c4ccc(Cl)cc4)no3)cc2)CN1Cc1ccco1 10.1021/acs.jmedchem.2c00508
164886639 3336 None 18 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assay
ChEMBL 462 6 1 6 4.6 O=C1CC(C(=O)Nc2ccc(c3nc(c4ccc(Cl)cc4)no3)cc2)CN1Cc1ccco1 10.1021/acs.jmedchem.2c00508
CHEMBL5207128 3336 None 18 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assay
ChEMBL 462 6 1 6 4.6 O=C1CC(C(=O)Nc2ccc(c3nc(c4ccc(Cl)cc4)no3)cc2)CN1Cc1ccco1 10.1021/acs.jmedchem.2c00508
CHEMBL2030700 211614 None 0 Human Functional pIC50 = 8.4 8.4 3 2
Agonist activity at RXFP3 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs by beta galactosidase reporter gene assayAgonist activity at RXFP3 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs by beta galactosidase reporter gene assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CN)C(C)C)CSSC[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)O)CSSC[C@@H](C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](C(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm201505p
165117350 191422 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assay
ChEMBL 467 7 1 6 4.3 CCc1ccc(-c2noc(-c3ccc(NC(=O)C4CC(=O)N(Cc5cccnc5)C4)cc3)n2)cc1 10.1021/acs.jmedchem.2c00508
CHEMBL5191322 191422 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assay
ChEMBL 467 7 1 6 4.3 CCc1ccc(-c2noc(-c3ccc(NC(=O)C4CC(=O)N(Cc5cccnc5)C4)cc3)n2)cc1 10.1021/acs.jmedchem.2c00508
165117356 190480 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assay
ChEMBL 458 6 1 6 4.8 Cc1ccc(-c2noc(-c3ccc(NC(=O)C4CC(=O)N(Cc5ccsc5)C4)cc3)n2)cc1 10.1021/acs.jmedchem.2c00508
CHEMBL5177224 190480 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assay
ChEMBL 458 6 1 6 4.8 Cc1ccc(-c2noc(-c3ccc(NC(=O)C4CC(=O)N(Cc5ccsc5)C4)cc3)n2)cc1 10.1021/acs.jmedchem.2c00508
12120 3336 None 18 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding incubated for 1 hr by [35S]GTP-gammaS binding assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding incubated for 1 hr by [35S]GTP-gammaS binding assay
ChEMBL 462 6 1 6 4.6 O=C1CC(C(=O)Nc2ccc(c3nc(c4ccc(Cl)cc4)no3)cc2)CN1Cc1ccco1 10.1021/acs.jmedchem.2c00508
164886639 3336 None 18 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding incubated for 1 hr by [35S]GTP-gammaS binding assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding incubated for 1 hr by [35S]GTP-gammaS binding assay
ChEMBL 462 6 1 6 4.6 O=C1CC(C(=O)Nc2ccc(c3nc(c4ccc(Cl)cc4)no3)cc2)CN1Cc1ccco1 10.1021/acs.jmedchem.2c00508
CHEMBL5207128 3336 None 18 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding incubated for 1 hr by [35S]GTP-gammaS binding assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding incubated for 1 hr by [35S]GTP-gammaS binding assay
ChEMBL 462 6 1 6 4.6 O=C1CC(C(=O)Nc2ccc(c3nc(c4ccc(Cl)cc4)no3)cc2)CN1Cc1ccco1 10.1021/acs.jmedchem.2c00508
165117358 192182 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assay
ChEMBL 442 6 1 6 4.3 Cc1ccc(-c2noc(-c3ccc(NC(=O)C4CC(=O)N(Cc5ccco5)C4)cc3)n2)cc1 10.1021/acs.jmedchem.2c00508
CHEMBL5202737 192182 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assay
ChEMBL 442 6 1 6 4.3 Cc1ccc(-c2noc(-c3ccc(NC(=O)C4CC(=O)N(Cc5ccco5)C4)cc3)n2)cc1 10.1021/acs.jmedchem.2c00508
50747793 190293 None 6 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding incubated for 1 hr by [35S]GTP-gammaS binding assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding incubated for 1 hr by [35S]GTP-gammaS binding assay
ChEMBL 452 6 1 5 4.7 Cc1ccc(-c2noc(-c3ccc(NC(=O)C4CC(=O)N(Cc5ccccc5)C4)cc3)n2)cc1 10.1021/acs.jmedchem.2c00508
CHEMBL5174194 190293 None 6 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding incubated for 1 hr by [35S]GTP-gammaS binding assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding incubated for 1 hr by [35S]GTP-gammaS binding assay
ChEMBL 452 6 1 5 4.7 Cc1ccc(-c2noc(-c3ccc(NC(=O)C4CC(=O)N(Cc5ccccc5)C4)cc3)n2)cc1 10.1021/acs.jmedchem.2c00508
165117365 190260 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assay
ChEMBL 470 6 1 5 4.8 Cc1ccc(-c2noc(-c3ccc(NC(=O)C4CC(=O)N(Cc5ccc(F)cc5)C4)cc3)n2)cc1 10.1021/acs.jmedchem.2c00508
CHEMBL5173667 190260 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assay
ChEMBL 470 6 1 5 4.8 Cc1ccc(-c2noc(-c3ccc(NC(=O)C4CC(=O)N(Cc5ccc(F)cc5)C4)cc3)n2)cc1 10.1021/acs.jmedchem.2c00508
CHEMBL2030701 211615 None 0 Human Functional pIC50 = 8.3 8.3 1 2
Agonist activity at RXFP3 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs by beta galactosidase reporter gene assayAgonist activity at RXFP3 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation after 6 hrs by beta galactosidase reporter gene assay
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CCCNC(=N)N)CSSC[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)O)CSSC[C@@H](C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](C(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm201505p
53242372 191042 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assay
ChEMBL 2620 84 43 34 -11.3 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H](N)CCCNC(=N)N)C(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)[C@@H](C)O)[C@@H](C)CC)C(C)C 10.1021/acs.jmedchem.2c00508
CHEMBL5185575 191042 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assay
ChEMBL 2620 84 43 34 -11.3 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H](N)CCCNC(=N)N)C(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)[C@@H](C)O)[C@@H](C)CC)C(C)C 10.1021/acs.jmedchem.2c00508
165117357 190498 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assay
ChEMBL 458 6 1 6 4.8 Cc1ccc(-c2noc(-c3ccc(NC(=O)C4CC(=O)N(Cc5cccs5)C4)cc3)n2)cc1 10.1021/acs.jmedchem.2c00508
CHEMBL5177511 190498 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assay
ChEMBL 458 6 1 6 4.8 Cc1ccc(-c2noc(-c3ccc(NC(=O)C4CC(=O)N(Cc5cccs5)C4)cc3)n2)cc1 10.1021/acs.jmedchem.2c00508
165117366 191335 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as inhibition of relaxin-3 stimulated ERK1/2 phosphorylation preincubated for 15 mins followed by relaxin-3 addition for 5 minsAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as inhibition of relaxin-3 stimulated ERK1/2 phosphorylation preincubated for 15 mins followed by relaxin-3 addition for 5 mins
ChEMBL 473 6 1 6 4.4 O=C(Nc1ccc(-c2nc(-c3ccc(Cl)cc3)no2)cc1)C1CC(=O)N(Cc2cccnc2)C1 10.1021/acs.jmedchem.2c00508
CHEMBL5189833 191335 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as inhibition of relaxin-3 stimulated ERK1/2 phosphorylation preincubated for 15 mins followed by relaxin-3 addition for 5 minsAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as inhibition of relaxin-3 stimulated ERK1/2 phosphorylation preincubated for 15 mins followed by relaxin-3 addition for 5 mins
ChEMBL 473 6 1 6 4.4 O=C(Nc1ccc(-c2nc(-c3ccc(Cl)cc3)no2)cc1)C1CC(=O)N(Cc2cccnc2)C1 10.1021/acs.jmedchem.2c00508
50747793 190293 None 6 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assay
ChEMBL 452 6 1 5 4.7 Cc1ccc(-c2noc(-c3ccc(NC(=O)C4CC(=O)N(Cc5ccccc5)C4)cc3)n2)cc1 10.1021/acs.jmedchem.2c00508
CHEMBL5174194 190293 None 6 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assay
ChEMBL 452 6 1 5 4.7 Cc1ccc(-c2noc(-c3ccc(NC(=O)C4CC(=O)N(Cc5ccccc5)C4)cc3)n2)cc1 10.1021/acs.jmedchem.2c00508
165117374 190317 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assay
ChEMBL 469 7 1 7 3.8 COc1ccc(-c2noc(-c3ccc(NC(=O)C4CC(=O)N(Cc5cccnc5)C4)cc3)n2)cc1 10.1021/acs.jmedchem.2c00508
CHEMBL5174579 190317 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assay
ChEMBL 469 7 1 7 3.8 COc1ccc(-c2noc(-c3ccc(NC(=O)C4CC(=O)N(Cc5cccnc5)C4)cc3)n2)cc1 10.1021/acs.jmedchem.2c00508
95740887 190844 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assay
ChEMBL 452 6 1 5 4.7 Cc1ccc(-c2noc(-c3ccc(NC(=O)[C@H]4CC(=O)N(Cc5ccccc5)C4)cc3)n2)cc1 10.1021/acs.jmedchem.2c00508
CHEMBL5182611 190844 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assay
ChEMBL 452 6 1 5 4.7 Cc1ccc(-c2noc(-c3ccc(NC(=O)[C@H]4CC(=O)N(Cc5ccccc5)C4)cc3)n2)cc1 10.1021/acs.jmedchem.2c00508
168270002 190062 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assay
ChEMBL 445 6 1 6 4.2 O=C(Nc1ccc(-c2nc(C3CCCCC3)no2)cc1)C1CC(=O)N(Cc2cccnc2)C1 10.1021/acs.jmedchem.2c00508
CHEMBL5170512 190062 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assay
ChEMBL 445 6 1 6 4.2 O=C(Nc1ccc(-c2nc(C3CCCCC3)no2)cc1)C1CC(=O)N(Cc2cccnc2)C1 10.1021/acs.jmedchem.2c00508
95740886 192573 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assay
ChEMBL 452 6 1 5 4.7 Cc1ccc(-c2noc(-c3ccc(NC(=O)[C@@H]4CC(=O)N(Cc5ccccc5)C4)cc3)n2)cc1 10.1021/acs.jmedchem.2c00508
CHEMBL5208662 192573 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assay
ChEMBL 452 6 1 5 4.7 Cc1ccc(-c2noc(-c3ccc(NC(=O)[C@@H]4CC(=O)N(Cc5ccccc5)C4)cc3)n2)cc1 10.1021/acs.jmedchem.2c00508
53242372 191042 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as inhibition of relaxin-3 stimulated ERK1/2 phosphorylation preincubated for 15 mins followed by relaxin-3 addition for 5 minsAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as inhibition of relaxin-3 stimulated ERK1/2 phosphorylation preincubated for 15 mins followed by relaxin-3 addition for 5 mins
ChEMBL 2620 84 43 34 -11.3 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H](N)CCCNC(=N)N)C(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)[C@@H](C)O)[C@@H](C)CC)C(C)C 10.1021/acs.jmedchem.2c00508
CHEMBL5185575 191042 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as inhibition of relaxin-3 stimulated ERK1/2 phosphorylation preincubated for 15 mins followed by relaxin-3 addition for 5 minsAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as inhibition of relaxin-3 stimulated ERK1/2 phosphorylation preincubated for 15 mins followed by relaxin-3 addition for 5 mins
ChEMBL 2620 84 43 34 -11.3 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H](N)CCCNC(=N)N)C(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)[C@@H](C)O)[C@@H](C)CC)C(C)C 10.1021/acs.jmedchem.2c00508
165117377 191413 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assay
ChEMBL 482 7 1 6 4.7 COc1ccc(CN2CC(C(=O)Nc3ccc(-c4nc(-c5ccc(C)cc5)no4)cc3)CC2=O)cc1 10.1021/acs.jmedchem.2c00508
CHEMBL5191162 191413 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assay
ChEMBL 482 7 1 6 4.7 COc1ccc(CN2CC(C(=O)Nc3ccc(-c4nc(-c5ccc(C)cc5)no4)cc3)CC2=O)cc1 10.1021/acs.jmedchem.2c00508
165117335 190069 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assay
ChEMBL 466 6 1 5 5.0 Cc1ccc(CN2CC(C(=O)Nc3ccc(-c4nc(-c5ccc(C)cc5)no4)cc3)CC2=O)cc1 10.1021/acs.jmedchem.2c00508
CHEMBL5170646 190069 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assayAntagonist activity at human RXFP3 expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation measured after 30 mins in presence of relaxin-3 by TR-FRET assay
ChEMBL 466 6 1 5 5.0 Cc1ccc(CN2CC(C(=O)Nc3ccc(-c4nc(-c5ccc(C)cc5)no4)cc3)CC2=O)cc1 10.1021/acs.jmedchem.2c00508
11907 4086 None 0 Human Functional pEC50 = 5.6 5.6 13 2
Determined in a cAMP accumulation assayDetermined in a cAMP accumulation assay
Guide to Pharmacology 577 14 5 8 3.3 CC(C)(CCc1ccc(NS(=O)(=O)c2ccccc2)cc1)NCC(O)COc1cc(NS(=O)(=O)C)c(O)cc1 34946593
162679545 4086 None 0 Human Functional pEC50 = 5.6 5.6 13 2
Determined in a cAMP accumulation assayDetermined in a cAMP accumulation assay
Guide to Pharmacology 577 14 5 8 3.3 CC(C)(CCc1ccc(NS(=O)(=O)c2ccccc2)cc1)NCC(O)COc1cc(NS(=O)(=O)C)c(O)cc1 34946593
11906 965 None 7 Human Functional pEC50 = 8.5 8.5 -1 2
Receptor activation via cAMP assayReceptor activation via cAMP assay
Guide to Pharmacology 402 6 4 5 2.8 C(#N)c1cc2c(c[nH]c2c(c1)C)/C=N/NC(=N)NCCc1ccc(C(=O)OC)cc1 34855388
162679544 965 None 7 Human Functional pEC50 = 8.5 8.5 -1 2
Receptor activation via cAMP assayReceptor activation via cAMP assay
Guide to Pharmacology 402 6 4 5 2.8 C(#N)c1cc2c(c[nH]c2c(c1)C)/C=N/NC(=N)NCCc1ccc(C(=O)OC)cc1 34855388
CHEMBL5089949 965 None 7 Human Functional pEC50 = 8.5 8.5 -1 2
Receptor activation via cAMP assayReceptor activation via cAMP assay
Guide to Pharmacology 402 6 4 5 2.8 C(#N)c1cc2c(c[nH]c2c(c1)C)/C=N/NC(=N)NCCc1ccc(C(=O)OC)cc1 34855388
56953333 18 None 0 Human Functional pEC50 = 6.1 6.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology 603 7 2 2 8.8 COc1ccc2c(c1)c(CCN(C(=O)Nc1cc(cc(c1)C(F)(F)F)C(F)(F)F)Cc1ccc(c(c1)Cl)Cl)c[nH]2 22347403
8343 18 None 0 Human Functional pEC50 = 6.1 6.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology 603 7 2 2 8.8 COc1ccc2c(c1)c(CCN(C(=O)Nc1cc(cc(c1)C(F)(F)F)C(F)(F)F)Cc1ccc(c(c1)Cl)Cl)c[nH]2 22347403
1989 3305 None 0 Human Functional pEC50 = 7.7 7.7 -467 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20159943
1989 3305 None 0 Human Functional pEC50 = 7.7 7.7 -467 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 24641548
11460 1115 None 0 Human Functional pEC50 = 7.9 7.9 -8 2
UnclassifiedUnclassified
Guide to Pharmacology 363 6 5 3 3.4 CCc1cc(O)cc2c1[nH]cc2/C=N/NC(=N)NCCc1ccc(cc1)C 30824200
155817523 1115 None 0 Human Functional pEC50 = 7.9 7.9 -8 2
UnclassifiedUnclassified
Guide to Pharmacology 363 6 5 3 3.4 CCc1cc(O)cc2c1[nH]cc2/C=N/NC(=N)NCCc1ccc(cc1)C 30824200
3907 3273 None 0 Human Functional pEC50 = 9.0 9.0 -5 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 24641548
1990 3307 None 0 Human Functional pEC50 = 9.1 9.1 1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17351017
1990 3307 None 0 Human Functional pEC50 = 9.1 9.1 1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18434306
1990 3307 None 0 Human Functional pEC50 = 9.1 9.1 1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20159943
1990 3307 None 0 Human Functional pEC50 = 9.1 9.1 1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 22257012
1990 3307 None 0 Human Functional pEC50 = 9.1 9.1 1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 24641548
8336 2536 None 0 Human Functional pEC50 = 9.4 9.4 51 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 22257012
11909 1782 None 0 Human Functional pIC50 = 10.1 10.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 28607363
3907 3273 None 0 Rat Functional pIC50 = 10.1 10.1 5 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 25496752
12120 3336 None 18 Human Functional pIC50 = 5.6 5.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology 462 6 1 6 4.6 O=C1CC(C(=O)Nc2ccc(c3nc(c4ccc(Cl)cc4)no3)cc2)CN1Cc1ccco1 35594150
164886639 3336 None 18 Human Functional pIC50 = 5.6 5.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology 462 6 1 6 4.6 O=C1CC(C(=O)Nc2ccc(c3nc(c4ccc(Cl)cc4)no3)cc2)CN1Cc1ccco1 35594150
CHEMBL5207128 3336 None 18 Human Functional pIC50 = 5.6 5.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology 462 6 1 6 4.6 O=C1CC(C(=O)Nc2ccc(c3nc(c4ccc(Cl)cc4)no3)cc2)CN1Cc1ccco1 35594150
1997 3309 None 0 Human Functional pIC50 = 6.9 6.9 -1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14522968
11910 1907 None 0 Human Functional pIC50 = 7.5 7.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 27498038
11910 1907 None 0 Human Functional pIC50 = 7.5 7.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 31220339
3907 3273 None 0 Human Functional pIC50 = 8.1 8.1 -5 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 25496752
11908 1908 None 0 Human Functional pIC50 = 8.5 8.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 27464307
3907 3273 None 0 Human Functional pIC50 = 9.2 9.2 -5 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17606621
3907 3273 None 0 Rat Functional pIC50 = 9.2 9.2 5 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 25496752
1998 3274 None 0 Human Functional pIC50 = 9.3 9.3 -2 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15465925
1998 3274 None 0 Human Functional pIC50 = 9.3 9.3 -2 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 23135160
3907 3273 None 0 Human Functional pIC50 = 9.4 9.4 -5 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 25496752
1990 3307 None 0 Human Functional pIC50 None 9.5 9.5 1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14522968
1990 3307 None 0 Human Functional pIC50 None 9.5 9.5 1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15367576
11923 3308 None 0 Rat Functional pIC50 ~ 8 8.0 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 23456488


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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
Sel. page Common
name		 GPCRdb
ID		 Reference
ligand		 Vendors

 Species

 Assay
Type		 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
155554720 174708 None 0 Human Binding pEC50 = 9.9 9.9 1 2
Agonist activity at human RXFP3 receptor expressed in CHOK1 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by alphascreen surefire assayAgonist activity at human RXFP3 receptor expressed in CHOK1 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by alphascreen surefire assay
ChEMBL 2117 55 33 26 -6.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@](C)(NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(C)=O)CCC/C=C/CCC[C@@](C)(C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)[C@@H](C)O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/acs.jmedchem.6b00265
CHEMBL4557279 174708 None 0 Human Binding pEC50 = 9.9 9.9 1 2
Agonist activity at human RXFP3 receptor expressed in CHOK1 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by alphascreen surefire assayAgonist activity at human RXFP3 receptor expressed in CHOK1 cells assessed as ERK1/2 phosphorylation incubated for 5 mins by alphascreen surefire assay
ChEMBL 2117 55 33 26 -6.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@](C)(NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(C)=O)CCC/C=C/CCC[C@@](C)(C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)[C@@H](C)O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/acs.jmedchem.6b00265
155513302 169850 None 0 Human Binding pKi = 7.0 7.0 1 2
Displacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assayDisplacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assay
ChEMBL 2386 65 38 29 -7.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@](C)(NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CCC/C=C/CCC[C@@](C)(C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)[C@@H](C)O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/acs.jmedchem.6b00265
CHEMBL4438620 169850 None 0 Human Binding pKi = 7.0 7.0 1 2
Displacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assayDisplacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assay
ChEMBL 2386 65 38 29 -7.2 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@](C)(NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)CCC/C=C/CCC[C@@](C)(C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)[C@@H](C)O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/acs.jmedchem.6b00265
155549840 173999 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assayDisplacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assay
ChEMBL 2344 64 38 29 -7.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@](C)(NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CCCNC(=N)N)CCC/C=C/CCC[C@@](C)(C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)[C@@H](C)O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/acs.jmedchem.6b00265
CHEMBL4540069 173999 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assayDisplacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assay
ChEMBL 2344 64 38 29 -7.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@](C)(NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CCCNC(=N)N)CCC/C=C/CCC[C@@](C)(C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)[C@@H](C)O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/acs.jmedchem.6b00265
162661135 181613 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of Eu-labeled H3B1-22R from RXFP3 (unknown origin) stably expressed in CHO-K1 cells by competition binding assayDisplacement of Eu-labeled H3B1-22R from RXFP3 (unknown origin) stably expressed in CHO-K1 cells by competition binding assay
ChEMBL 4679 97 71 64 -15.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)N[C@H](COC(N)=O)Cc2c[nH]c3ccccc23)C(C)C)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC1=O 10.1021/acsmedchemlett.0c00456
CHEMBL4764969 181613 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of Eu-labeled H3B1-22R from RXFP3 (unknown origin) stably expressed in CHO-K1 cells by competition binding assayDisplacement of Eu-labeled H3B1-22R from RXFP3 (unknown origin) stably expressed in CHO-K1 cells by competition binding assay
ChEMBL 4679 97 71 64 -15.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)N[C@H](COC(N)=O)Cc2c[nH]c3ccccc23)C(C)C)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC1=O 10.1021/acsmedchemlett.0c00456
CHEMBL2030702 211616 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of europium-labelled H3 relaxin-B chain/INSL-5 chain from RXFP3 expressed in CHO-K1 cellsDisplacement of europium-labelled H3 relaxin-B chain/INSL-5 chain from RXFP3 expressed in CHO-K1 cells
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](N)CSSC[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)O)CSSC[C@@H](C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](C(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm201505p
53242372 191042 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [125I]R3/I5 from human RXFP3 expressed in CHO-K1 cells membrane assessed as inhibition constant incubated for 1 hr by microplate scintillation counting analysisDisplacement of [125I]R3/I5 from human RXFP3 expressed in CHO-K1 cells membrane assessed as inhibition constant incubated for 1 hr by microplate scintillation counting analysis
ChEMBL 2620 84 43 34 -11.3 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H](N)CCCNC(=N)N)C(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)[C@@H](C)O)[C@@H](C)CC)C(C)C 10.1021/acs.jmedchem.2c00508
CHEMBL5185575 191042 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [125I]R3/I5 from human RXFP3 expressed in CHO-K1 cells membrane assessed as inhibition constant incubated for 1 hr by microplate scintillation counting analysisDisplacement of [125I]R3/I5 from human RXFP3 expressed in CHO-K1 cells membrane assessed as inhibition constant incubated for 1 hr by microplate scintillation counting analysis
ChEMBL 2620 84 43 34 -11.3 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H](N)CCCNC(=N)N)C(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)[C@@H](C)O)[C@@H](C)CC)C(C)C 10.1021/acs.jmedchem.2c00508
CHEMBL2030700 211614 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of europium-labelled H3 relaxin-B chain/INSL-5 chain from RXFP3 expressed in CHO-K1 cellsDisplacement of europium-labelled H3 relaxin-B chain/INSL-5 chain from RXFP3 expressed in CHO-K1 cells
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CN)C(C)C)CSSC[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)O)CSSC[C@@H](C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](C(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm201505p
CHEMBL2030701 211615 None 0 Human Binding pKi = 7.0 7.0 - 1
Displacement of europium-labelled H3 relaxin-B chain/INSL-5 chain from RXFP3 expressed in CHO-K1 cellsDisplacement of europium-labelled H3 relaxin-B chain/INSL-5 chain from RXFP3 expressed in CHO-K1 cells
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CCCNC(=N)N)CSSC[C@H](N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)O)CSSC[C@@H](C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](C(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm201505p
155511404 169656 None 0 Human Binding pKi = 6.8 6.8 2 2
Displacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assayDisplacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assay
ChEMBL 2075 54 33 26 -6.7 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@](C)(NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](N)CO)CCC/C=C/CCC[C@@](C)(C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)[C@@H](C)O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/acs.jmedchem.6b00265
CHEMBL4435599 169656 None 0 Human Binding pKi = 6.8 6.8 2 2
Displacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assayDisplacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assay
ChEMBL 2075 54 33 26 -6.7 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@](C)(NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](N)CO)CCC/C=C/CCC[C@@](C)(C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)[C@@H](C)O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/acs.jmedchem.6b00265
155566939 175995 None 0 Human Binding pKi = 5.8 5.8 - 1
Displacement of [125I]-R3/I5 from human RXFP3 expressed in CHOK1 cell membranes by radioligand binding assayDisplacement of [125I]-R3/I5 from human RXFP3 expressed in CHOK1 cell membranes by radioligand binding assay
ChEMBL 417 6 4 3 4.5 COc1cc(C)c2[nH]cc(/C=N/NC(=N)NCCc3ccc(Cl)c(Cl)c3)c2c1 10.1016/j.bmcl.2019.02.013
CHEMBL4586446 175995 None 0 Human Binding pKi = 5.8 5.8 - 1
Displacement of [125I]-R3/I5 from human RXFP3 expressed in CHOK1 cell membranes by radioligand binding assayDisplacement of [125I]-R3/I5 from human RXFP3 expressed in CHOK1 cell membranes by radioligand binding assay
ChEMBL 417 6 4 3 4.5 COc1cc(C)c2[nH]cc(/C=N/NC(=N)NCCc3ccc(Cl)c(Cl)c3)c2c1 10.1016/j.bmcl.2019.02.013
162664973 182170 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of Eu-labeled H3B1-22R from RXFP3 (unknown origin) stably expressed in CHO-K1 cells by competition binding assayDisplacement of Eu-labeled H3B1-22R from RXFP3 (unknown origin) stably expressed in CHO-K1 cells by competition binding assay
ChEMBL 4778 100 72 66 -16.9 CC[C@H](C)[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)OC[C@H](NC(C)=O)C(N)=O)C(C)C)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC1=O 10.1021/acsmedchemlett.0c00456
CHEMBL4781389 182170 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of Eu-labeled H3B1-22R from RXFP3 (unknown origin) stably expressed in CHO-K1 cells by competition binding assayDisplacement of Eu-labeled H3B1-22R from RXFP3 (unknown origin) stably expressed in CHO-K1 cells by competition binding assay
ChEMBL 4778 100 72 66 -16.9 CC[C@H](C)[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)OC[C@H](NC(C)=O)C(N)=O)C(C)C)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC1=O 10.1021/acsmedchemlett.0c00456
162675340 183565 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of Eu-labeled H3B1-22R from RXFP3 (unknown origin) stably expressed in CHO-K1 cells by competition binding assayDisplacement of Eu-labeled H3B1-22R from RXFP3 (unknown origin) stably expressed in CHO-K1 cells by competition binding assay
ChEMBL 4649 96 71 63 -16.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C(C)C)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC1=O 10.1021/acsmedchemlett.0c00456
CHEMBL4799017 183565 None 0 Human Binding pKi = 6.7 6.7 - 1
Displacement of Eu-labeled H3B1-22R from RXFP3 (unknown origin) stably expressed in CHO-K1 cells by competition binding assayDisplacement of Eu-labeled H3B1-22R from RXFP3 (unknown origin) stably expressed in CHO-K1 cells by competition binding assay
ChEMBL 4649 96 71 63 -16.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)N[C@@H](Cc2c[nH]c3ccccc23)C(N)=O)C(C)C)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC1=O 10.1021/acsmedchemlett.0c00456
CHEMBL2030698 211612 None 0 Human Binding pKi = 5.7 5.7 - 1
Displacement of europium-labelled H3 relaxin-B chain/INSL-5 chain from RXFP3 expressed in CHO-K1 cellsDisplacement of europium-labelled H3 relaxin-B chain/INSL-5 chain from RXFP3 expressed in CHO-K1 cells
ChEMBL None None None None 10.1021/jm201505p
155519131 170460 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assayDisplacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assay
ChEMBL 2542 70 40 31 -8.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@](C)(NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CNC(C)=O)C(C)C)CCC/C=C/CCC[C@@](C)(C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)[C@@H](C)O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/acs.jmedchem.6b00265
CHEMBL4447532 170460 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assayDisplacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assay
ChEMBL 2542 70 40 31 -8.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@](C)(NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CNC(C)=O)C(C)C)CCC/C=C/CCC[C@@](C)(C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)[C@@H](C)O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/acs.jmedchem.6b00265
155566939 175995 None 0 Human Binding pKi = 5.6 5.6 - 1
Displacement of [125I]R3/I5 from human RXFP3 expressed in human CHO-K1 cells incubated for 1 hr by microplate scintillation counting analysisDisplacement of [125I]R3/I5 from human RXFP3 expressed in human CHO-K1 cells incubated for 1 hr by microplate scintillation counting analysis
ChEMBL 417 6 4 3 4.5 COc1cc(C)c2[nH]cc(/C=N/NC(=N)NCCc3ccc(Cl)c(Cl)c3)c2c1 10.1021/acs.jmedchem.1c01081
CHEMBL4586446 175995 None 0 Human Binding pKi = 5.6 5.6 - 1
Displacement of [125I]R3/I5 from human RXFP3 expressed in human CHO-K1 cells incubated for 1 hr by microplate scintillation counting analysisDisplacement of [125I]R3/I5 from human RXFP3 expressed in human CHO-K1 cells incubated for 1 hr by microplate scintillation counting analysis
ChEMBL 417 6 4 3 4.5 COc1cc(C)c2[nH]cc(/C=N/NC(=N)NCCc3ccc(Cl)c(Cl)c3)c2c1 10.1021/acs.jmedchem.1c01081
155562158 175812 None 0 Human Binding pKi = 5.6 5.6 - 1
Displacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assayDisplacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assay
ChEMBL 2099 55 33 28 -8.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(C)=O)CCSSCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)[C@@H](C)O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/acs.jmedchem.6b00265
CHEMBL4582266 175812 None 0 Human Binding pKi = 5.6 5.6 - 1
Displacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assayDisplacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assay
ChEMBL 2099 55 33 28 -8.0 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(C)=O)CCSSCC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)[C@@H](C)O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/acs.jmedchem.6b00265
CHEMBL2030699 211613 None 0 Human Binding pKi = 5.6 5.6 - 1
Displacement of europium-labelled H3 relaxin-B chain/INSL-5 chain from RXFP3 expressed in CHO-K1 cellsDisplacement of europium-labelled H3 relaxin-B chain/INSL-5 chain from RXFP3 expressed in CHO-K1 cells
ChEMBL None None None None 10.1021/jm201505p
CHEMBL5094670 217998 None 0 Human Binding pKi = 6.6 6.6 - 1
Displacement of [125I]R3/I5 from human RXFP3 expressed in human CHO-K1 cells incubated for 1 hr by microplate scintillation counting analysisDisplacement of [125I]R3/I5 from human RXFP3 expressed in human CHO-K1 cells incubated for 1 hr by microplate scintillation counting analysis
ChEMBL None None None COc1cc(C)c2[nH]cc(/C=N/NC(=N)NCCc3ccc(C#N)cc3)c2c1 10.1021/acs.jmedchem.1c01081
138319674 173287 None 7 Human Binding pKi = 6.6 6.6 - 1
Displacement of [125I]R3/I5 from human RXFP3 expressed in human CHO-K1 cells incubated for 1 hr by microplate scintillation counting analysisDisplacement of [125I]R3/I5 from human RXFP3 expressed in human CHO-K1 cells incubated for 1 hr by microplate scintillation counting analysis
ChEMBL 383 6 5 3 3.8 CCc1cc(O)cc2c(/C=N/NC(=N)NCCc3ccc(Cl)cc3)c[nH]c12 10.1021/acs.jmedchem.1c01081
CHEMBL4522365 173287 None 7 Human Binding pKi = 6.6 6.6 - 1
Displacement of [125I]R3/I5 from human RXFP3 expressed in human CHO-K1 cells incubated for 1 hr by microplate scintillation counting analysisDisplacement of [125I]R3/I5 from human RXFP3 expressed in human CHO-K1 cells incubated for 1 hr by microplate scintillation counting analysis
ChEMBL 383 6 5 3 3.8 CCc1cc(O)cc2c(/C=N/NC(=N)NCCc3ccc(Cl)cc3)c[nH]c12 10.1021/acs.jmedchem.1c01081
155554720 174708 None 0 Human Binding pKi = 6.6 6.6 1 2
Displacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assayDisplacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assay
ChEMBL 2117 55 33 26 -6.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@](C)(NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(C)=O)CCC/C=C/CCC[C@@](C)(C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)[C@@H](C)O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/acs.jmedchem.6b00265
CHEMBL4557279 174708 None 0 Human Binding pKi = 6.6 6.6 1 2
Displacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assayDisplacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assay
ChEMBL 2117 55 33 26 -6.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@](C)(NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(C)=O)CCC/C=C/CCC[C@@](C)(C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)[C@@H](C)O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/acs.jmedchem.6b00265
16214672 173964 None 0 Human Binding pKi = 5.5 5.5 -1 2
Displacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assayDisplacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assay
ChEMBL 3041 95 49 39 -10.9 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CS)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H](N)CCCNC(=N)N)C(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CS)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)O)[C@@H](C)CC)C(C)C 10.1021/acs.jmedchem.6b00265
CHEMBL4539255 173964 None 0 Human Binding pKi = 5.5 5.5 -1 2
Displacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assayDisplacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assay
ChEMBL 3041 95 49 39 -10.9 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CS)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@@H](N)CCCNC(=N)N)C(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CS)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)O)[C@@H](C)CC)C(C)C 10.1021/acs.jmedchem.6b00265
CHEMBL2030691 211609 None 0 Human Binding pKi = 5.5 5.5 - 1
Displacement of europium-labelled H3 relaxin-B chain/INSL-5 chain from RXFP3 expressed in CHO-K1 cellsDisplacement of europium-labelled H3 relaxin-B chain/INSL-5 chain from RXFP3 expressed in CHO-K1 cells
ChEMBL None None None None 10.1021/jm201505p
162661752 181951 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of Eu-labeled H3B1-22R from RXFP3 (unknown origin) stably expressed in CHO-K1 cells by competition binding assayDisplacement of Eu-labeled H3B1-22R from RXFP3 (unknown origin) stably expressed in CHO-K1 cells by competition binding assay
ChEMBL 4636 96 71 63 -15.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)N[C@H](CO)Cc2c[nH]c3ccccc23)C(C)C)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC1=O 10.1021/acsmedchemlett.0c00456
CHEMBL4778498 181951 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of Eu-labeled H3B1-22R from RXFP3 (unknown origin) stably expressed in CHO-K1 cells by competition binding assayDisplacement of Eu-labeled H3B1-22R from RXFP3 (unknown origin) stably expressed in CHO-K1 cells by competition binding assay
ChEMBL 4636 96 71 63 -15.5 CC[C@H](C)[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)N[C@H](CO)Cc2c[nH]c3ccccc23)C(C)C)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC1=O 10.1021/acsmedchemlett.0c00456
CHEMBL2030697 211611 None 0 Human Binding pKi = 5.5 5.5 - 1
Displacement of europium-labelled H3 relaxin-B chain/INSL-5 chain from RXFP3 expressed in CHO-K1 cellsDisplacement of europium-labelled H3 relaxin-B chain/INSL-5 chain from RXFP3 expressed in CHO-K1 cells
ChEMBL None None None None 10.1021/jm201505p
162659068 181364 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of Eu-labeled H3B1-22R from RXFP3 (unknown origin) stably expressed in CHO-K1 cells by competition binding assayDisplacement of Eu-labeled H3B1-22R from RXFP3 (unknown origin) stably expressed in CHO-K1 cells by competition binding assay
ChEMBL 4650 96 71 63 -15.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)C(C)C)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC1=O 10.1021/acsmedchemlett.0c00456
CHEMBL4761849 181364 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of Eu-labeled H3B1-22R from RXFP3 (unknown origin) stably expressed in CHO-K1 cells by competition binding assayDisplacement of Eu-labeled H3B1-22R from RXFP3 (unknown origin) stably expressed in CHO-K1 cells by competition binding assay
ChEMBL 4650 96 71 63 -15.4 CC[C@H](C)[C@@H]1NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H]2CCCN2C(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)C(C)C)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC1=O 10.1021/acsmedchemlett.0c00456
155567021 175974 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assayDisplacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assay
ChEMBL 2372 66 38 29 -6.9 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@]1(C)CCC/C=C\CCC[C@@](C)(C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](C(C)C)NC1=O 10.1021/acs.jmedchem.6b00265
CHEMBL4586048 175974 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assayDisplacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assay
ChEMBL 2372 66 38 29 -6.9 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@]1(C)CCC/C=C\CCC[C@@](C)(C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](C(C)C)NC1=O 10.1021/acs.jmedchem.6b00265
155526100 171199 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assayDisplacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assay
ChEMBL 2414 67 38 29 -6.7 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@]1(C)CCC/C=C\CCC[C@@](C)(C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](C(C)C)NC1=O 10.1021/acs.jmedchem.6b00265
CHEMBL4457624 171199 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assayDisplacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assay
ChEMBL 2414 67 38 29 -6.7 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@]1(C)CCC/C=C\CCC[C@@](C)(C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](C(C)C)NC1=O 10.1021/acs.jmedchem.6b00265
11906 965 None 7 Human Binding pKi = 7.2 7.2 - 1
Displacement of [125I]R3/I5 from human RXFP3 expressed in human CHO-K1 cells incubated for 1 hr by microplate scintillation counting analysisDisplacement of [125I]R3/I5 from human RXFP3 expressed in human CHO-K1 cells incubated for 1 hr by microplate scintillation counting analysis
ChEMBL 402 6 4 5 2.8 C(#N)c1cc2c(c[nH]c2c(c1)C)/C=N/NC(=N)NCCc1ccc(C(=O)OC)cc1 10.1021/acs.jmedchem.1c01081
162679544 965 None 7 Human Binding pKi = 7.2 7.2 - 1
Displacement of [125I]R3/I5 from human RXFP3 expressed in human CHO-K1 cells incubated for 1 hr by microplate scintillation counting analysisDisplacement of [125I]R3/I5 from human RXFP3 expressed in human CHO-K1 cells incubated for 1 hr by microplate scintillation counting analysis
ChEMBL 402 6 4 5 2.8 C(#N)c1cc2c(c[nH]c2c(c1)C)/C=N/NC(=N)NCCc1ccc(C(=O)OC)cc1 10.1021/acs.jmedchem.1c01081
CHEMBL5089949 965 None 7 Human Binding pKi = 7.2 7.2 - 1
Displacement of [125I]R3/I5 from human RXFP3 expressed in human CHO-K1 cells incubated for 1 hr by microplate scintillation counting analysisDisplacement of [125I]R3/I5 from human RXFP3 expressed in human CHO-K1 cells incubated for 1 hr by microplate scintillation counting analysis
ChEMBL 402 6 4 5 2.8 C(#N)c1cc2c(c[nH]c2c(c1)C)/C=N/NC(=N)NCCc1ccc(C(=O)OC)cc1 10.1021/acs.jmedchem.1c01081
CHEMBL2030696 211610 None 0 Human Binding pKi = 6.1 6.1 - 1
Displacement of europium-labelled H3 relaxin-B chain/INSL-5 chain from RXFP3 expressed in CHO-K1 cellsDisplacement of europium-labelled H3 relaxin-B chain/INSL-5 chain from RXFP3 expressed in CHO-K1 cells
ChEMBL None None None None 10.1021/jm201505p
155538336 172489 None 0 Human Binding pKi = 7.0 7.0 2 2
Displacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assayDisplacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assay
ChEMBL 2500 69 40 31 -8.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@](C)(NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CN)C(C)C)CCC/C=C/CCC[C@@](C)(C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)[C@@H](C)O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/acs.jmedchem.6b00265
CHEMBL4476408 172489 None 0 Human Binding pKi = 7.0 7.0 2 2
Displacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assayDisplacement of Eu-H3/15 from human RXFP3 receptor expressed in CHOK1 cells by time-resolved fluorescent whole cell binding assay
ChEMBL 2500 69 40 31 -8.1 CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@](C)(NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)CN)C(C)C)CCC/C=C/CCC[C@@](C)(C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)NCC(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)O)[C@@H](C)O)[C@@H](C)CC)C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/acs.jmedchem.6b00265
1989 3305 None 0 Human Binding pKd = 10 10.0 1 3
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20159943
8342 1602 None 0 Human Binding pKd = 7.6 7.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 25792111
4374 1604 None 0 Human Binding pKd = 8.3 8.3 3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21384867
11912 1468 None 0 Human Binding pKd = 8.7 8.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 22187146
11911 3275 None 0 Human Binding pKd = 9.2 9.2 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 29770870
4374 1604 None 0 Human Binding pKd = 9.3 9.3 3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21384867
4374 1604 None 0 Human Binding pKd = 9.3 9.3 3 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 22257012
11906 965 None 7 Human Binding pKi = 7.2 7.2 - 1
Receptor bindingReceptor binding
Guide to Pharmacology 402 6 4 5 2.8 C(#N)c1cc2c(c[nH]c2c(c1)C)/C=N/NC(=N)NCCc1ccc(C(=O)OC)cc1 34855388
162679544 965 None 7 Human Binding pKi = 7.2 7.2 - 1
Receptor bindingReceptor binding
Guide to Pharmacology 402 6 4 5 2.8 C(#N)c1cc2c(c[nH]c2c(c1)C)/C=N/NC(=N)NCCc1ccc(C(=O)OC)cc1 34855388
CHEMBL5089949 965 None 7 Human Binding pKi = 7.2 7.2 - 1
Receptor bindingReceptor binding
Guide to Pharmacology 402 6 4 5 2.8 C(#N)c1cc2c(c[nH]c2c(c1)C)/C=N/NC(=N)NCCc1ccc(C(=O)OC)cc1 34855388
11459 563 None 0 Human Binding pKi = 5.9 5.9 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 32133341
8337 3310 None 0 Human Binding pKi = 6.6 6.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17351017
2000 2048 None 0 Human Binding pKi = 7.0 7.0 -10 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18582868
11461 3272 None 0 Human Binding pKi = 7.4 7.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21384867
8326 2537 None 0 Human Binding pKi = 7.6 7.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 22257012
11461 3272 None 0 Human Binding pKi = 7.7 7.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 25792111
8336 2536 None 0 Human Binding pKi = 7.9 7.9 5 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 22257012
8336 2536 None 0 Human Binding pKi = 7.9 7.9 5 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 28864207
1990 3307 None 0 Human Binding pKi = 8.4 8.4 -3 4
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17351017
1990 3307 None 0 Human Binding pKi = 8.4 8.4 -3 4
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18434306
1990 3307 None 0 Human Binding pKi = 8.4 8.4 -3 4
UnclassifiedUnclassified
Guide to Pharmacology None None None None 22257012
3907 3273 None 0 Human Binding pKi = 8.5 8.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21384867