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Found 138 hits Enz. Inhib. hit(s) with Target = 'Pyroglutamylated RFamide peptide receptor' AND taxid = 9606   
Target
(Institution)
LigandTarget
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kJ/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50347818
PNG
(CHEMBL1802413 | P518)
Show SMILES CC(C)C[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CO)NC(=O)[C@@H](N)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O
Show InChI InChI=1S/C127H195N37O37/c1-66(2)49-83(160-124(200)94-35-24-48-164(94)101(176)62-144-110(186)91(63-165)163-125(201)104(132)70(8)168)108(184)142-61-100(175)148-90(57-96(131)171)121(197)157-84(50-67(3)4)116(192)145-69(7)106(182)149-80(40-42-102(177)178)114(190)154-81(41-43-103(179)180)115(191)156-85(51-68(5)6)117(193)159-89(56-95(130)170)109(185)143-60-99(174)147-87(55-74-36-38-75(169)39-37-74)119(195)161-92(64-166)122(198)153-78(33-22-46-138-126(134)135)112(188)151-77(32-19-21-45-129)111(187)150-76(31-18-20-44-128)107(183)141-58-97(172)140-59-98(173)146-86(53-72-27-14-10-15-28-72)118(194)162-93(65-167)123(199)158-88(54-73-29-16-11-17-30-73)120(196)152-79(34-23-47-139-127(136)137)113(189)155-82(105(133)181)52-71-25-12-9-13-26-71/h9-17,25-30,36-39,66-70,76-94,104,165-169H,18-24,31-35,40-65,128-129,132H2,1-8H3,(H2,130,170)(H2,131,171)(H2,133,181)(H,140,172)(H,141,183)(H,142,184)(H,143,185)(H,144,186)(H,145,192)(H,146,173)(H,147,174)(H,148,175)(H,149,182)(H,150,187)(H,151,188)(H,152,196)(H,153,198)(H,154,190)(H,155,189)(H,156,191)(H,157,197)(H,158,199)(H,159,193)(H,160,200)(H,161,195)(H,162,194)(H,163,201)(H,177,178)(H,179,180)(H4,134,135,138)(H4,136,137,139)/t69-,70+,76-,77-,78-,79-,80-,81-,82-,83-,84-,85-,86-,87-,88-,89-,90-,91-,92-,93-,94-,104-/m0/s1
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n/an/a 1.30n/an/an/an/an/an/a



INSERM

Curated by ChEMBL


Assay Description
Displacement of [125I]26RFa from human GPR103 expressed in HEK293 cells incubated for 1 h by gamma counter based method


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50020015
PNG
(CHEMBL3287814)
Show SMILES COc1ccc(NC(=N)c2ccc(Cl)cc2)cc1CSC1CCCC1
Show InChI InChI=1S/C20H23ClN2OS/c1-24-19-11-10-17(12-15(19)13-25-18-4-2-3-5-18)23-20(22)14-6-8-16(21)9-7-14/h6-12,18H,2-5,13H2,1H3,(H2,22,23)
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n/an/a 13n/an/an/an/an/an/a



AstraZeneca

Curated by ChEMBL


Assay Description
Antagonist activity at human GPR103 receptor assessed as inhibition of inositol-1-phosphate production by cell-based assay


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50020011
PNG
(CHEMBL3287810)
Show SMILES COc1ccc(NC(=N)c2ccccc2)cc1CSC1CCCC1
Show InChI InChI=1S/C20H24N2OS/c1-23-19-12-11-17(22-20(21)15-7-3-2-4-8-15)13-16(19)14-24-18-9-5-6-10-18/h2-4,7-8,11-13,18H,5-6,9-10,14H2,1H3,(H2,21,22)
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n/an/a 20n/an/an/an/an/an/a



AstraZeneca

Curated by ChEMBL


Assay Description
Antagonist activity at human GPR103 receptor assessed as inhibition of inositol-1-phosphate production by cell-based assay


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50020014
PNG
(CHEMBL3287813)
Show SMILES COc1ccc(NC(=N)c2ccc(Br)s2)cc1CSC1CCCC1
Show InChI InChI=1S/C18H21BrN2OS2/c1-22-15-7-6-13(21-18(20)16-8-9-17(19)24-16)10-12(15)11-23-14-4-2-3-5-14/h6-10,14H,2-5,11H2,1H3,(H2,20,21)
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AstraZeneca

Curated by ChEMBL


Assay Description
Antagonist activity at human GPR103 receptor assessed as inhibition of inositol-1-phosphate production by cell-based assay


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50020011
PNG
(CHEMBL3287810)
Show SMILES COc1ccc(NC(=N)c2ccccc2)cc1CSC1CCCC1
Show InChI InChI=1S/C20H24N2OS/c1-23-19-12-11-17(22-20(21)15-7-3-2-4-8-15)13-16(19)14-24-18-9-5-6-10-18/h2-4,7-8,11-13,18H,5-6,9-10,14H2,1H3,(H2,21,22)
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n/an/a 25n/an/an/an/an/an/a



AstraZeneca

Curated by ChEMBL


Assay Description
Displacement of [125I]-QRFP43 from human GPR103 receptor overexpressed in HEK membranes after 90 mins by liquid scintillation counting


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50045830
PNG
(CHEMBL3314362)
Show SMILES CN(C)Cc1cc2CCN(Cc2cc1C)C(=O)c1cc2cc(Cl)ccc2n1C
Show InChI InChI=1S/C23H26ClN3O/c1-15-9-19-14-27(8-7-16(19)10-18(15)13-25(2)3)23(28)22-12-17-11-20(24)5-6-21(17)26(22)4/h5-6,9-12H,7-8,13-14H2,1-4H3
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AstraZeneca

Curated by ChEMBL


Assay Description
Displacement of [125I]QRFP43 from human GPR103 receptor expressed in HEK cells after 90 mins incubation by scintillation counting


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50020015
PNG
(CHEMBL3287814)
Show SMILES COc1ccc(NC(=N)c2ccc(Cl)cc2)cc1CSC1CCCC1
Show InChI InChI=1S/C20H23ClN2OS/c1-24-19-11-10-17(12-15(19)13-25-18-4-2-3-5-18)23-20(22)14-6-8-16(21)9-7-14/h6-12,18H,2-5,13H2,1H3,(H2,22,23)
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AstraZeneca

Curated by ChEMBL


Assay Description
Displacement of [125I]-QRFP43 from human GPR103 receptor overexpressed in HEK membranes after 90 mins by liquid scintillation counting


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50045830
PNG
(CHEMBL3314362)
Show SMILES CN(C)Cc1cc2CCN(Cc2cc1C)C(=O)c1cc2cc(Cl)ccc2n1C
Show InChI InChI=1S/C23H26ClN3O/c1-15-9-19-14-27(8-7-16(19)10-18(15)13-25(2)3)23(28)22-12-17-11-20(24)5-6-21(17)26(22)4/h5-6,9-12H,7-8,13-14H2,1-4H3
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n/an/a 46n/an/an/an/an/an/a



AstraZeneca

Curated by ChEMBL


Assay Description
Inhibition of human GPR103 receptor expressed in CHOK1 cells by IP-1 assay


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50019982
PNG
(CHEMBL3287584)
Show SMILES COc1ccc(NC(=N)c2cccs2)cc1CSC1CCCC1
Show InChI InChI=1S/C18H22N2OS2/c1-21-16-9-8-14(20-18(19)17-7-4-10-22-17)11-13(16)12-23-15-5-2-3-6-15/h4,7-11,15H,2-3,5-6,12H2,1H3,(H2,19,20)
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n/an/a 50n/an/an/an/an/an/a



AstraZeneca

Curated by ChEMBL


Assay Description
Antagonist activity at human GPR103 receptor assessed as inhibition of inositol-1-phosphate production by cell-based assay


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50020012
PNG
(CHEMBL3287811)
Show SMILES COc1ccc(NC(=N)c2cc(C)cs2)cc1CSC1CCCC1
Show InChI InChI=1S/C19H24N2OS2/c1-13-9-18(24-11-13)19(20)21-15-7-8-17(22-2)14(10-15)12-23-16-5-3-4-6-16/h7-11,16H,3-6,12H2,1-2H3,(H2,20,21)
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AstraZeneca

Curated by ChEMBL


Assay Description
Antagonist activity at human GPR103 receptor assessed as inhibition of inositol-1-phosphate production by cell-based assay


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50045833
PNG
(CHEMBL3314349)
Show SMILES CN(C)Cc1ccc2CN(CCc2c1)C(=O)c1cc2cc(Cl)ccc2n1C
Show InChI InChI=1S/C22H24ClN3O/c1-24(2)13-15-4-5-17-14-26(9-8-16(17)10-15)22(27)21-12-18-11-19(23)6-7-20(18)25(21)3/h4-7,10-12H,8-9,13-14H2,1-3H3
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n/an/a 70n/an/an/an/an/an/a



AstraZeneca

Curated by ChEMBL


Assay Description
Displacement of [125I]QRFP43 from human GPR103 receptor expressed in HEK cells after 90 mins incubation by scintillation counting


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50045833
PNG
(CHEMBL3314349)
Show SMILES CN(C)Cc1ccc2CN(CCc2c1)C(=O)c1cc2cc(Cl)ccc2n1C
Show InChI InChI=1S/C22H24ClN3O/c1-24(2)13-15-4-5-17-14-26(9-8-16(17)10-15)22(27)21-12-18-11-19(23)6-7-20(18)25(21)3/h4-7,10-12H,8-9,13-14H2,1-3H3
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n/an/a 70n/an/an/an/an/an/a



AstraZeneca

Curated by ChEMBL


Assay Description
Inhibition of human GPR103 receptor expressed in CHOK1 cells by IP-1 assay


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50019983
PNG
(CHEMBL3287585)
Show SMILES COc1ccc(Cl)cc1NS(=O)(=O)c1ccc(OC)c2C[C@@H](CCc12)N(C)C
Show InChI InChI=1S/C20H25ClN2O4S/c1-23(2)14-6-7-15-16(12-14)18(26-3)9-10-20(15)28(24,25)22-17-11-13(21)5-8-19(17)27-4/h5,8-11,14,22H,6-7,12H2,1-4H3/t14-/m1/s1
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n/an/a 79n/an/an/an/an/an/a



AstraZeneca

Curated by ChEMBL


Assay Description
Antagonist activity at human GPR103 receptor assessed as inhibition of inositol-1-phosphate production by cell-based assay


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50019983
PNG
(CHEMBL3287585)
Show SMILES COc1ccc(Cl)cc1NS(=O)(=O)c1ccc(OC)c2C[C@@H](CCc12)N(C)C
Show InChI InChI=1S/C20H25ClN2O4S/c1-23(2)14-6-7-15-16(12-14)18(26-3)9-10-20(15)28(24,25)22-17-11-13(21)5-8-19(17)27-4/h5,8-11,14,22H,6-7,12H2,1-4H3/t14-/m1/s1
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n/an/a 79n/an/an/an/an/an/a



AstraZeneca

Curated by ChEMBL


Assay Description
Displacement of [125I]-QRFP43 from human GPR103 receptor overexpressed in HEK membranes after 90 mins by liquid scintillation counting


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50020010
PNG
(CHEMBL3287586)
Show SMILES COc1ccc(NC(=N)c2ccsc2)cc1CSC1CCCC1
Show InChI InChI=1S/C18H22N2OS2/c1-21-17-7-6-15(20-18(19)13-8-9-22-11-13)10-14(17)12-23-16-4-2-3-5-16/h6-11,16H,2-5,12H2,1H3,(H2,19,20)
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AstraZeneca

Curated by ChEMBL


Assay Description
Antagonist activity at human GPR103 receptor assessed as inhibition of inositol-1-phosphate production by cell-based assay


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50020012
PNG
(CHEMBL3287811)
Show SMILES COc1ccc(NC(=N)c2cc(C)cs2)cc1CSC1CCCC1
Show InChI InChI=1S/C19H24N2OS2/c1-13-9-18(24-11-13)19(20)21-15-7-8-17(22-2)14(10-15)12-23-16-5-3-4-6-16/h7-11,16H,3-6,12H2,1-2H3,(H2,20,21)
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AstraZeneca

Curated by ChEMBL


Assay Description
Displacement of [125I]-QRFP43 from human GPR103 receptor overexpressed in HEK membranes after 90 mins by liquid scintillation counting


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50045838
PNG
(CHEMBL3314358)
Show SMILES CC1CN(Cc2ccc(CN(C)C)cc12)C(=O)c1cc2cc(Br)ncc2n1C
Show InChI InChI=1/C22H25BrN4O/c1-14-11-27(13-16-6-5-15(7-18(14)16)12-25(2)3)22(28)19-8-17-9-21(23)24-10-20(17)26(19)4/h5-10,14H,11-13H2,1-4H3
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AstraZeneca

Curated by ChEMBL


Assay Description
Inhibition of human GPR103 receptor expressed in CHOK1 cells by IP-1 assay


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50020014
PNG
(CHEMBL3287813)
Show SMILES COc1ccc(NC(=N)c2ccc(Br)s2)cc1CSC1CCCC1
Show InChI InChI=1S/C18H21BrN2OS2/c1-22-15-7-6-13(21-18(20)16-8-9-17(19)24-16)10-12(15)11-23-14-4-2-3-5-14/h6-10,14H,2-5,11H2,1H3,(H2,20,21)
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AstraZeneca

Curated by ChEMBL


Assay Description
Displacement of [125I]-QRFP43 from human GPR103 receptor overexpressed in HEK membranes after 90 mins by liquid scintillation counting


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50020010
PNG
(CHEMBL3287586)
Show SMILES COc1ccc(NC(=N)c2ccsc2)cc1CSC1CCCC1
Show InChI InChI=1S/C18H22N2OS2/c1-21-17-7-6-15(20-18(19)13-8-9-22-11-13)10-14(17)12-23-16-4-2-3-5-16/h6-11,16H,2-5,12H2,1H3,(H2,19,20)
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AstraZeneca

Curated by ChEMBL


Assay Description
Displacement of [125I]-QRFP43 from human GPR103 receptor overexpressed in HEK membranes after 90 mins by liquid scintillation counting


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50045842
PNG
(CHEMBL3314354)
Show SMILES CN(C)Cc1ccc2CN(CCc2c1)C(=O)c1cc2cc(I)ncc2n1C
Show InChI InChI=1S/C21H23IN4O/c1-24(2)12-14-4-5-16-13-26(7-6-15(16)8-14)21(27)18-9-17-10-20(22)23-11-19(17)25(18)3/h4-5,8-11H,6-7,12-13H2,1-3H3
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AstraZeneca

Curated by ChEMBL


Assay Description
Inhibition of human GPR103 receptor expressed in CHOK1 cells by IP-1 assay


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50020013
PNG
(CHEMBL3287812)
Show SMILES COc1ccc(NC(=N)c2cc(Br)cs2)cc1CSC1CCCC1
Show InChI InChI=1S/C18H21BrN2OS2/c1-22-16-7-6-14(21-18(20)17-9-13(19)11-24-17)8-12(16)10-23-15-4-2-3-5-15/h6-9,11,15H,2-5,10H2,1H3,(H2,20,21)
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AstraZeneca

Curated by ChEMBL


Assay Description
Antagonist activity at human GPR103 receptor assessed as inhibition of inositol-1-phosphate production by cell-based assay


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50019982
PNG
(CHEMBL3287584)
Show SMILES COc1ccc(NC(=N)c2cccs2)cc1CSC1CCCC1
Show InChI InChI=1S/C18H22N2OS2/c1-21-16-9-8-14(20-18(19)17-7-4-10-22-17)11-13(16)12-23-15-5-2-3-6-15/h4,7-11,15H,2-3,5-6,12H2,1H3,(H2,19,20)
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AstraZeneca

Curated by ChEMBL


Assay Description
Displacement of [125I]-QRFP43 from human GPR103 receptor overexpressed in HEK membranes after 90 mins by liquid scintillation counting


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50019979
PNG
(CHEMBL3287833)
Show SMILES COc1ccc(NC(=N)c2ccccc2)cc1CCC1CCCC1
Show InChI InChI=1S/C21H26N2O/c1-24-20-14-13-19(23-21(22)17-9-3-2-4-10-17)15-18(20)12-11-16-7-5-6-8-16/h2-4,9-10,13-16H,5-8,11-12H2,1H3,(H2,22,23)
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AstraZeneca

Curated by ChEMBL


Assay Description
Displacement of [125I]-QRFP43 from human GPR103 receptor overexpressed in HEK membranes after 90 mins by liquid scintillation counting


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50045831
PNG
(CHEMBL3314352)
Show SMILES CN(C)Cc1ccc2CN(CCc2c1)C(=O)c1cc2cc(Br)ncc2n1C
Show InChI InChI=1S/C21H23BrN4O/c1-24(2)12-14-4-5-16-13-26(7-6-15(16)8-14)21(27)18-9-17-10-20(22)23-11-19(17)25(18)3/h4-5,8-11H,6-7,12-13H2,1-3H3
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AstraZeneca

Curated by ChEMBL


Assay Description
Inhibition of human GPR103 receptor expressed in CHOK1 cells by IP-1 assay


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50020020
PNG
(CHEMBL3287819)
Show SMILES COc1ccc(NC(=N)c2cccnc2)cc1CSC1CCCC1
Show InChI InChI=1S/C19H23N3OS/c1-23-18-9-8-16(22-19(20)14-5-4-10-21-12-14)11-15(18)13-24-17-6-2-3-7-17/h4-5,8-12,17H,2-3,6-7,13H2,1H3,(H2,20,22)
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AstraZeneca

Curated by ChEMBL


Assay Description
Antagonist activity at human GPR103 receptor assessed as inhibition of inositol-1-phosphate production by cell-based assay


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50020022
PNG
(CHEMBL3287821)
Show SMILES COc1ccc(N\C(=N\C)c2cccs2)cc1CSC1CCCC1
Show InChI InChI=1S/C19H24N2OS2/c1-20-19(18-8-5-11-23-18)21-15-9-10-17(22-2)14(12-15)13-24-16-6-3-4-7-16/h5,8-12,16H,3-4,6-7,13H2,1-2H3,(H,20,21)
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n/an/a 251n/an/an/an/an/an/a



AstraZeneca

Curated by ChEMBL


Assay Description
Antagonist activity at human GPR103 receptor assessed as inhibition of inositol-1-phosphate production by cell-based assay


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50045831
PNG
(CHEMBL3314352)
Show SMILES CN(C)Cc1ccc2CN(CCc2c1)C(=O)c1cc2cc(Br)ncc2n1C
Show InChI InChI=1S/C21H23BrN4O/c1-24(2)12-14-4-5-16-13-26(7-6-15(16)8-14)21(27)18-9-17-10-20(22)23-11-19(17)25(18)3/h4-5,8-11H,6-7,12-13H2,1-3H3
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AstraZeneca

Curated by ChEMBL


Assay Description
Displacement of [125I]QRFP43 from human GPR103 receptor expressed in HEK cells after 90 mins incubation by scintillation counting


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50019979
PNG
(CHEMBL3287833)
Show SMILES COc1ccc(NC(=N)c2ccccc2)cc1CCC1CCCC1
Show InChI InChI=1S/C21H26N2O/c1-24-20-14-13-19(23-21(22)17-9-3-2-4-10-17)15-18(20)12-11-16-7-5-6-8-16/h2-4,9-10,13-16H,5-8,11-12H2,1H3,(H2,22,23)
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AstraZeneca

Curated by ChEMBL


Assay Description
Antagonist activity at human GPR103 receptor assessed as inhibition of inositol-1-phosphate production by cell-based assay


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50045834
PNG
(CHEMBL3314361)
Show SMILES CC(N(C)C)c1ccc2CN(CCc2c1)C(=O)c1cc2cc(Cl)ncc2n1C
Show InChI InChI=1/C22H25ClN4O/c1-14(25(2)3)15-5-6-17-13-27(8-7-16(17)9-15)22(28)19-10-18-11-21(23)24-12-20(18)26(19)4/h5-6,9-12,14H,7-8,13H2,1-4H3
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AstraZeneca

Curated by ChEMBL


Assay Description
Inhibition of human GPR103 receptor expressed in CHOK1 cells by IP-1 assay


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50045837
PNG
(CHEMBL3314359)
Show SMILES CC1N(CCc2cc(CN(C)C)ccc12)C(=O)c1cc2cc(Cl)ncc2n1C
Show InChI InChI=1/C22H25ClN4O/c1-14-18-6-5-15(13-25(2)3)9-16(18)7-8-27(14)22(28)19-10-17-11-21(23)24-12-20(17)26(19)4/h5-6,9-12,14H,7-8,13H2,1-4H3
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AstraZeneca

Curated by ChEMBL


Assay Description
Inhibition of human GPR103 receptor expressed in CHOK1 cells by IP-1 assay


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50019976
PNG
(CHEMBL3287827)
Show SMILES Fc1ccc(NC(=N)c2cccs2)cc1CSC1CCCC1
Show InChI InChI=1S/C17H19FN2S2/c18-15-8-7-13(20-17(19)16-6-3-9-21-16)10-12(15)11-22-14-4-1-2-5-14/h3,6-10,14H,1-2,4-5,11H2,(H2,19,20)
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AstraZeneca

Curated by ChEMBL


Assay Description
Antagonist activity at human GPR103 receptor assessed as inhibition of inositol-1-phosphate production by cell-based assay


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50020020
PNG
(CHEMBL3287819)
Show SMILES COc1ccc(NC(=N)c2cccnc2)cc1CSC1CCCC1
Show InChI InChI=1S/C19H23N3OS/c1-23-18-9-8-16(22-19(20)14-5-4-10-21-12-14)11-15(18)13-24-17-6-2-3-7-17/h4-5,8-12,17H,2-3,6-7,13H2,1H3,(H2,20,22)
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AstraZeneca

Curated by ChEMBL


Assay Description
Displacement of [125I]-QRFP43 from human GPR103 receptor overexpressed in HEK membranes after 90 mins by liquid scintillation counting


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50045846
PNG
(CHEMBL3314350)
Show SMILES CN(C)Cc1ccc2CN(CCc2c1)C(=O)c1cc2cc(Cl)ncc2n1C
Show InChI InChI=1S/C21H23ClN4O/c1-24(2)12-14-4-5-16-13-26(7-6-15(16)8-14)21(27)18-9-17-10-20(22)23-11-19(17)25(18)3/h4-5,8-11H,6-7,12-13H2,1-3H3
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AstraZeneca

Curated by ChEMBL


Assay Description
Inhibition of human GPR103 receptor expressed in CHOK1 cells by IP-1 assay


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50020022
PNG
(CHEMBL3287821)
Show SMILES COc1ccc(N\C(=N\C)c2cccs2)cc1CSC1CCCC1
Show InChI InChI=1S/C19H24N2OS2/c1-20-19(18-8-5-11-23-18)21-15-9-10-17(22-2)14(12-15)13-24-16-6-3-4-7-16/h5,8-12,16H,3-4,6-7,13H2,1-2H3,(H,20,21)
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n/an/a 631n/an/an/an/an/an/a



AstraZeneca

Curated by ChEMBL


Assay Description
Displacement of [125I]-QRFP43 from human GPR103 receptor overexpressed in HEK membranes after 90 mins by liquid scintillation counting


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50045836
PNG
(CHEMBL3314360)
Show SMILES CC1Cc2cc(CN(C)C)ccc2CN1C(=O)c1cc2cc(Cl)ncc2n1C
Show InChI InChI=1/C22H25ClN4O/c1-14-7-17-8-15(12-25(2)3)5-6-16(17)13-27(14)22(28)19-9-18-10-21(23)24-11-20(18)26(19)4/h5-6,8-11,14H,7,12-13H2,1-4H3
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AstraZeneca

Curated by ChEMBL


Assay Description
Inhibition of human GPR103 receptor expressed in CHOK1 cells by IP-1 assay


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50019974
PNG
(CHEMBL3287825)
Show SMILES N=C(Nc1cccc(CSC2CCCC2)c1)c1cccs1
Show InChI InChI=1S/C17H20N2S2/c18-17(16-9-4-10-20-16)19-14-6-3-5-13(11-14)12-21-15-7-1-2-8-15/h3-6,9-11,15H,1-2,7-8,12H2,(H2,18,19)
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AstraZeneca

Curated by ChEMBL


Assay Description
Antagonist activity at human GPR103 receptor assessed as inhibition of inositol-1-phosphate production by cell-based assay


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50045830
PNG
(CHEMBL3314362)
Show SMILES CN(C)Cc1cc2CCN(Cc2cc1C)C(=O)c1cc2cc(Cl)ccc2n1C
Show InChI InChI=1S/C23H26ClN3O/c1-15-9-19-14-27(8-7-16(19)10-18(15)13-25(2)3)23(28)22-12-17-11-20(24)5-6-21(17)26(22)4/h5-6,9-12H,7-8,13-14H2,1-4H3
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AstraZeneca

Curated by ChEMBL


Assay Description
Inhibition of human GPR103 receptor expressed in CHOK1 cells by IP-1 assay


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50019973
PNG
(CHEMBL3287824)
Show SMILES COc1ccc(cc1CSC1CCCC1)C(=N)Nc1ccccc1
Show InChI InChI=1S/C20H24N2OS/c1-23-19-12-11-15(20(21)22-17-7-3-2-4-8-17)13-16(19)14-24-18-9-5-6-10-18/h2-4,7-8,11-13,18H,5-6,9-10,14H2,1H3,(H2,21,22)
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AstraZeneca

Curated by ChEMBL


Assay Description
Antagonist activity at human GPR103 receptor assessed as inhibition of inositol-1-phosphate production by cell-based assay


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50019977
PNG
(CHEMBL3287828)
Show SMILES Clc1ccc(NC(=N)c2cccs2)cc1CSC1CCCC1
Show InChI InChI=1S/C17H19ClN2S2/c18-15-8-7-13(20-17(19)16-6-3-9-21-16)10-12(15)11-22-14-4-1-2-5-14/h3,6-10,14H,1-2,4-5,11H2,(H2,19,20)
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AstraZeneca

Curated by ChEMBL


Assay Description
Antagonist activity at human GPR103 receptor assessed as inhibition of inositol-1-phosphate production by cell-based assay


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50019976
PNG
(CHEMBL3287827)
Show SMILES Fc1ccc(NC(=N)c2cccs2)cc1CSC1CCCC1
Show InChI InChI=1S/C17H19FN2S2/c18-15-8-7-13(20-17(19)16-6-3-9-21-16)10-12(15)11-22-14-4-1-2-5-14/h3,6-10,14H,1-2,4-5,11H2,(H2,19,20)
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n/an/a 1.26E+3n/an/an/an/an/an/a



AstraZeneca

Curated by ChEMBL


Assay Description
Displacement of [125I]-QRFP43 from human GPR103 receptor overexpressed in HEK membranes after 90 mins by liquid scintillation counting


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50019975
PNG
(CHEMBL3287826)
Show SMILES Cc1ccc(NC(=N)c2cccs2)cc1CSC1CCCC1
Show InChI InChI=1S/C18H22N2S2/c1-13-8-9-15(20-18(19)17-7-4-10-21-17)11-14(13)12-22-16-5-2-3-6-16/h4,7-11,16H,2-3,5-6,12H2,1H3,(H2,19,20)
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n/an/a 1.59E+3n/an/an/an/an/an/a



AstraZeneca

Curated by ChEMBL


Assay Description
Antagonist activity at human GPR103 receptor assessed as inhibition of inositol-1-phosphate production by cell-based assay


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50019980
PNG
(CHEMBL3287834)
Show SMILES COc1ccc(NC(=N)c2ccccc2)cc1CSc1ccccc1
Show InChI InChI=1S/C21H20N2OS/c1-24-20-13-12-18(23-21(22)16-8-4-2-5-9-16)14-17(20)15-25-19-10-6-3-7-11-19/h2-14H,15H2,1H3,(H2,22,23)
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AstraZeneca

Curated by ChEMBL


Assay Description
Antagonist activity at human GPR103 receptor assessed as inhibition of inositol-1-phosphate production by cell-based assay


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50020019
PNG
(CHEMBL3287818)
Show SMILES COc1ccc(NC(=N)c2ccncc2)cc1CSC1CCCC1
Show InChI InChI=1S/C19H23N3OS/c1-23-18-7-6-16(22-19(20)14-8-10-21-11-9-14)12-15(18)13-24-17-4-2-3-5-17/h6-12,17H,2-5,13H2,1H3,(H2,20,22)
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AstraZeneca

Curated by ChEMBL


Assay Description
Antagonist activity at human GPR103 receptor assessed as inhibition of inositol-1-phosphate production by cell-based assay


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50396422
PNG
(CHEMBL2170403)
Show SMILES NC(N)=NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CN(CC(O)CO)NC(=O)[C@H](Cc1ccccc1)NC(=O)CN1CCNCC1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O
Show InChI InChI=1S/C44H62N12O8/c45-40(61)35(23-30-11-4-1-5-12-30)53-41(62)34(17-10-18-49-44(46)47)52-42(63)36(24-31-13-6-2-7-14-31)50-39(60)28-56(26-33(58)29-57)54-43(64)37(25-32-15-8-3-9-16-32)51-38(59)27-55-21-19-48-20-22-55/h1-9,11-16,33-37,48,57-58H,10,17-29H2,(H2,45,61)(H,50,60)(H,51,59)(H,52,63)(H,53,62)(H,54,64)(H4,46,47,49)/t33?,34-,35-,36-,37-/m0/s1
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n/an/a 1.99E+3n/an/an/an/an/an/a



INSERM

Curated by ChEMBL


Assay Description
Displacement of [125I]26RFa from human GPR103 expressed in HEK293 cells incubated for 1 h by gamma counter based method


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50020024
PNG
(CHEMBL3287829)
Show SMILES FC(F)(F)Oc1ccc(NC(=N)c2cccs2)cc1CSC1CCCC1
Show InChI InChI=1S/C18H19F3N2OS2/c19-18(20,21)24-15-8-7-13(23-17(22)16-6-3-9-25-16)10-12(15)11-26-14-4-1-2-5-14/h3,6-10,14H,1-2,4-5,11H2,(H2,22,23)
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n/an/a 2.00E+3n/an/an/an/an/an/a



AstraZeneca

Curated by ChEMBL


Assay Description
Antagonist activity at human GPR103 receptor assessed as inhibition of inositol-1-phosphate production by cell-based assay


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50019981
PNG
(CHEMBL3287835)
Show SMILES COc1ccc(NC(=N)c2ccccc2)cc1CNC(=O)C1CCCC1
Show InChI InChI=1S/C21H25N3O2/c1-26-19-12-11-18(24-20(22)15-7-3-2-4-8-15)13-17(19)14-23-21(25)16-9-5-6-10-16/h2-4,7-8,11-13,16H,5-6,9-10,14H2,1H3,(H2,22,24)(H,23,25)
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n/an/a 2.51E+3n/an/an/an/an/an/a



AstraZeneca

Curated by ChEMBL


Assay Description
Antagonist activity at human GPR103 receptor assessed as inhibition of inositol-1-phosphate production by cell-based assay


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50019978
PNG
(CHEMBL3287832)
Show SMILES COc1ccc(NC(=N)c2cccs2)cc1COC1CCCC1
Show InChI InChI=1S/C18H22N2O2S/c1-21-16-9-8-14(20-18(19)17-7-4-10-23-17)11-13(16)12-22-15-5-2-3-6-15/h4,7-11,15H,2-3,5-6,12H2,1H3,(H2,19,20)
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n/an/a 2.51E+3n/an/an/an/an/an/a



AstraZeneca

Curated by ChEMBL


Assay Description
Antagonist activity at human GPR103 receptor assessed as inhibition of inositol-1-phosphate production by cell-based assay


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50019974
PNG
(CHEMBL3287825)
Show SMILES N=C(Nc1cccc(CSC2CCCC2)c1)c1cccs1
Show InChI InChI=1S/C17H20N2S2/c18-17(16-9-4-10-20-16)19-14-6-3-5-13(11-14)12-21-15-7-1-2-8-15/h3-6,9-11,15H,1-2,7-8,12H2,(H2,18,19)
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n/an/a 2.51E+3n/an/an/an/an/an/a



AstraZeneca

Curated by ChEMBL


Assay Description
Displacement of [125I]-QRFP43 from human GPR103 receptor overexpressed in HEK membranes after 90 mins by liquid scintillation counting


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50020018
PNG
(CHEMBL3287817)
Show SMILES COc1ccc(NC(=N)c2nccs2)cc1CSC1CCCC1
Show InChI InChI=1S/C17H21N3OS2/c1-21-15-7-6-13(20-16(18)17-19-8-9-22-17)10-12(15)11-23-14-4-2-3-5-14/h6-10,14H,2-5,11H2,1H3,(H2,18,20)
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n/an/a 2.51E+3n/an/an/an/an/an/a



AstraZeneca

Curated by ChEMBL


Assay Description
Antagonist activity at human GPR103 receptor assessed as inhibition of inositol-1-phosphate production by cell-based assay


Citation and Details
More data for this
Ligand-Target Pair
Pyroglutamylated RFamide peptide receptor


(Homo sapiens)
BDBM50019984
PNG
(CHEMBL528724 | GNF-Pf-1241)
Show SMILES Cc1cc2nc(NC(N)=N)nc(C)c2cc1C
Show InChI InChI=1S/C12H15N5/c1-6-4-9-8(3)15-12(17-11(13)14)16-10(9)5-7(6)2/h4-5H,1-3H3,(H4,13,14,15,16,17)
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n/an/a 2.51E+3n/an/an/an/an/an/a



AstraZeneca

Curated by ChEMBL


Assay Description
Antagonist activity at human GPR103 receptor assessed as inhibition of inositol-1-phosphate production by cell-based assay


Citation and Details
More data for this
Ligand-Target Pair
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