Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
Sel. page Common
name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Potency)		 # tested GPCRs
(Potency)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
4064 9213 0 None -3 3 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 525 25 4 8 4.7 CCCCCCCCCCCCCCCCCC(=O)OC[C@H](COP(=O)(OC[C@@H](C(=O)O)N)O)O 16460680
4064 9213 0 None -3 3 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 525 25 4 8 4.7 CCCCCCCCCCCCCCCCCC(=O)OC[C@H](COP(=O)(OC[C@@H](C(=O)O)N)O)O 22343749
42607474 9213 0 None -3 3 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 525 25 4 8 4.7 CCCCCCCCCCCCCCCCCC(=O)OC[C@H](COP(=O)(OC[C@@H](C(=O)O)N)O)O 16460680
42607474 9213 0 None -3 3 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 525 25 4 8 4.7 CCCCCCCCCCCCCCCCCC(=O)OC[C@H](COP(=O)(OC[C@@H](C(=O)O)N)O)O 22343749
CHEMBL582985 9213 0 None -3 3 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 525 25 4 8 4.7 CCCCCCCCCCCCCCCCCC(=O)OC[C@H](COP(=O)(OC[C@@H](C(=O)O)N)O)O 16460680
CHEMBL582985 9213 0 None -3 3 Human 6.7 pEC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 525 25 4 8 4.7 CCCCCCCCCCCCCCCCCC(=O)OC[C@H](COP(=O)(OC[C@@H](C(=O)O)N)O)O 22343749
4064 9213 0 None 1 3 Mouse 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 525 25 4 8 4.7 CCCCCCCCCCCCCCCCCC(=O)OC[C@H](COP(=O)(OC[C@@H](C(=O)O)N)O)O 16460680
42607474 9213 0 None 1 3 Mouse 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 525 25 4 8 4.7 CCCCCCCCCCCCCCCCCC(=O)OC[C@H](COP(=O)(OC[C@@H](C(=O)O)N)O)O 16460680
CHEMBL582985 9213 0 None 1 3 Mouse 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 525 25 4 8 4.7 CCCCCCCCCCCCCCCCCC(=O)OC[C@H](COP(=O)(OC[C@@H](C(=O)O)N)O)O 16460680
12947 10886 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 582 9 2 4 6.0 OC(=O)C1(CCN(CC1)C(=O)C2=CC=C(C=C2)C3=CC(Cl)=CC=C3)NC(=O)CC4=CC=C(OCC5=CC=CC=C5)C=C4 21193033
169422747 10886 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 582 9 2 4 6.0 OC(=O)C1(CCN(CC1)C(=O)C2=CC=C(C=C2)C3=CC(Cl)=CC=C3)NC(=O)CC4=CC=C(OCC5=CC=CC=C5)C=C4 21193033


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Ligands Receptor Assay information Chemical information
Sel. page Common
name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Affinity)		 # tested GPCRs
(Affinity)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
78319665 187272 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 587 21 3 9 4.8 CCCCCCCCCCCOc1ccccc1CCC(=O)O[C@@H]1CCOC[C@H]1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4753103 187272 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 587 21 3 9 4.8 CCCCCCCCCCCOc1ccccc1CCC(=O)O[C@@H]1CCOC[C@H]1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
78319665 187272 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 587 21 3 9 4.8 CCCCCCCCCCCOc1ccccc1CCC(=O)O[C@@H]1CCOC[C@H]1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4753103 187272 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 587 21 3 9 4.8 CCCCCCCCCCCOc1ccccc1CCC(=O)O[C@@H]1CCOC[C@H]1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
78319665 187272 0 None - 0 Mouse 9.1 pEC50 = 9.1 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 587 21 3 9 4.8 CCCCCCCCCCCOc1ccccc1CCC(=O)O[C@@H]1CCOC[C@H]1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4753103 187272 0 None - 0 Mouse 9.1 pEC50 = 9.1 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 587 21 3 9 4.8 CCCCCCCCCCCOc1ccccc1CCC(=O)O[C@@H]1CCOC[C@H]1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
78319665 187272 0 None - 0 Mouse 9.1 pEC50 = 9.1 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 587 21 3 9 4.8 CCCCCCCCCCCOc1ccccc1CCC(=O)O[C@@H]1CCOC[C@H]1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4753103 187272 0 None - 0 Mouse 9.1 pEC50 = 9.1 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 587 21 3 9 4.8 CCCCCCCCCCCOc1ccccc1CCC(=O)O[C@@H]1CCOC[C@H]1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
90322737 188270 0 None - 0 Mouse 8.0 pEC50 = 8.0 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 537 25 3 8 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](COC)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4764776 188270 0 None - 0 Mouse 8.0 pEC50 = 8.0 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 537 25 3 8 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](COC)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
137659825 166164 0 None - 0 Mouse 7.0 pEC50 = 7 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 699 17 3 9 5.1 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(I)cc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL4100630 166164 0 None - 0 Mouse 7.0 pEC50 = 7 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 699 17 3 9 5.1 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(I)cc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
145948884 174279 0 None - 0 Mouse 7.0 pEC50 = 7 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 563 23 3 8 5.7 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H]1OCCC[C@H]1OP(=O)(O)OC[C@@H](N)C(=O)O 10.1021/acs.jmedchem.5b01925
CHEMBL4299658 174279 0 None - 0 Mouse 7.0 pEC50 = 7 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 563 23 3 8 5.7 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H]1OCCC[C@H]1OP(=O)(O)OC[C@@H](N)C(=O)O 10.1021/acs.jmedchem.5b01925
137659825 166164 0 None - 0 Mouse 7.0 pEC50 = 7.0 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 699 17 3 9 5.1 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(I)cc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL4100630 166164 0 None - 0 Mouse 7.0 pEC50 = 7.0 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 699 17 3 9 5.1 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(I)cc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
137660195 165933 0 None - 0 Mouse 7.0 pEC50 = 7.0 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 641 17 3 9 5.8 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(Cl)c(Cl)c2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL4098171 165933 0 None - 0 Mouse 7.0 pEC50 = 7.0 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 641 17 3 9 5.8 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(Cl)c(Cl)c2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
78319747 147433 0 None - 0 Mouse 7.0 pEC50 = 7.0 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 601 22 3 9 5.2 CCCCCCCCCCCOc1ccccc1CCC(=O)OC[C@H]1OCCC[C@H]1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.5b01925
CHEMBL3814763 147433 0 None - 0 Mouse 7.0 pEC50 = 7.0 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 601 22 3 9 5.2 CCCCCCCCCCCOc1ccccc1CCC(=O)OC[C@H]1OCCC[C@H]1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.5b01925
90322737 188270 0 None - 0 Mouse 8.0 pEC50 = 8.0 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 537 25 3 8 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](COC)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4764776 188270 0 None - 0 Mouse 8.0 pEC50 = 8.0 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 537 25 3 8 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](COC)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
162666591 189126 0 None - 0 Mouse 7.9 pEC50 = 7.9 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 561 26 3 8 5.1 C#CCOC[C@H](COC(=O)CCCCCCC/C=C\CCCCCCCC)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4784581 189126 0 None - 0 Mouse 7.9 pEC50 = 7.9 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 561 26 3 8 5.1 C#CCOC[C@H](COC(=O)CCCCCCC/C=C\CCCCCCCC)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
137660195 165933 0 None - 0 Mouse 7.0 pEC50 = 7.0 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 641 17 3 9 5.8 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(Cl)c(Cl)c2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL4098171 165933 0 None - 0 Mouse 7.0 pEC50 = 7.0 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 641 17 3 9 5.8 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(Cl)c(Cl)c2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
78319747 147433 0 None - 0 Mouse 7.0 pEC50 = 7.0 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 601 22 3 9 5.2 CCCCCCCCCCCOc1ccccc1CCC(=O)OC[C@H]1OCCC[C@H]1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.5b01925
CHEMBL3814763 147433 0 None - 0 Mouse 7.0 pEC50 = 7.0 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 601 22 3 9 5.2 CCCCCCCCCCCOc1ccccc1CCC(=O)OC[C@H]1OCCC[C@H]1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.5b01925
137640237 163586 0 None - 0 Mouse 6.9 pEC50 = 6.9 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 607 17 3 9 5.1 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(Cl)cc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL4071116 163586 0 None - 0 Mouse 6.9 pEC50 = 6.9 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 607 17 3 9 5.1 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(Cl)cc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
137637812 162821 0 None - 0 Mouse 6.9 pEC50 = 6.9 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 591 17 3 9 4.6 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(F)cc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL4062480 162821 0 None - 0 Mouse 6.9 pEC50 = 6.9 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 591 17 3 9 4.6 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(F)cc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
127051444 147460 0 None - 0 Mouse 6.9 pEC50 = 6.9 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 663 16 3 10 5.3 N[C@@H](COP(=O)(O)OC[C@H]1OCCC[C@H]1OC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(Cl)cc2)c1)C(=O)O 10.1021/acs.jmedchem.5b01925
CHEMBL3815141 147460 0 None - 0 Mouse 6.9 pEC50 = 6.9 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 663 16 3 10 5.3 N[C@@H](COP(=O)(O)OC[C@H]1OCCC[C@H]1OC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(Cl)cc2)c1)C(=O)O 10.1021/acs.jmedchem.5b01925
162666591 189126 0 None - 0 Mouse 7.9 pEC50 = 7.9 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 561 26 3 8 5.1 C#CCOC[C@H](COC(=O)CCCCCCC/C=C\CCCCCCCC)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4784581 189126 0 None - 0 Mouse 7.9 pEC50 = 7.9 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 561 26 3 8 5.1 C#CCOC[C@H](COC(=O)CCCCCCC/C=C\CCCCCCCC)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
137637812 162821 0 None - 0 Mouse 6.9 pEC50 = 6.9 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 591 17 3 9 4.6 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(F)cc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL4062480 162821 0 None - 0 Mouse 6.9 pEC50 = 6.9 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 591 17 3 9 4.6 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(F)cc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
137640237 163586 0 None - 0 Mouse 6.9 pEC50 = 6.9 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 607 17 3 9 5.1 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(Cl)cc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL4071116 163586 0 None - 0 Mouse 6.9 pEC50 = 6.9 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 607 17 3 9 5.1 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(Cl)cc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
127051444 147460 0 None - 0 Mouse 6.9 pEC50 = 6.9 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 663 16 3 10 5.3 N[C@@H](COP(=O)(O)OC[C@H]1OCCC[C@H]1OC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(Cl)cc2)c1)C(=O)O 10.1021/acs.jmedchem.5b01925
CHEMBL3815141 147460 0 None - 0 Mouse 6.9 pEC50 = 6.9 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 663 16 3 10 5.3 N[C@@H](COP(=O)(O)OC[C@H]1OCCC[C@H]1OC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(Cl)cc2)c1)C(=O)O 10.1021/acs.jmedchem.5b01925
137637516 162736 0 None - 0 Mouse 5.9 pEC50 = 5.9 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 567 21 3 9 4.1 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCCCCCCOc1ccccc1)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL4061305 162736 0 None - 0 Mouse 5.9 pEC50 = 5.9 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 567 21 3 9 4.1 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCCCCCCOc1ccccc1)C(=O)O 10.1021/acs.jmedchem.7b00693
137646672 164457 0 None - 0 Mouse 5.9 pEC50 = 5.9 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 607 17 3 9 5.1 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2Cl)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL4081667 164457 0 None - 0 Mouse 5.9 pEC50 = 5.9 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 607 17 3 9 5.1 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2Cl)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
137637516 162736 0 None - 0 Mouse 5.9 pEC50 = 5.9 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 567 21 3 9 4.1 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCCCCCCOc1ccccc1)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL4061305 162736 0 None - 0 Mouse 5.9 pEC50 = 5.9 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 567 21 3 9 4.1 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCCCCCCOc1ccccc1)C(=O)O 10.1021/acs.jmedchem.7b00693
137646672 164457 0 None - 0 Mouse 5.9 pEC50 = 5.9 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 607 17 3 9 5.1 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2Cl)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL4081667 164457 0 None - 0 Mouse 5.9 pEC50 = 5.9 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 607 17 3 9 5.1 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2Cl)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
137656253 165357 0 None - 0 Mouse 5.9 pEC50 = 5.9 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 571 17 3 8 4.3 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Cc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL4091854 165357 0 None - 0 Mouse 5.9 pEC50 = 5.9 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 571 17 3 8 4.3 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Cc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
162656636 187726 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 617 19 3 10 4.5 CCOC[C@H](COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4758243 187726 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 617 19 3 10 4.5 CCOC[C@H](COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
137656253 165357 0 None - 0 Mouse 5.9 pEC50 = 5.9 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 571 17 3 8 4.3 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Cc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL4091854 165357 0 None - 0 Mouse 5.9 pEC50 = 5.9 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 571 17 3 8 4.3 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Cc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
52926278 127933 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 495 22 4 8 3.7 CCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
CHEMBL3577144 127933 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 495 22 4 8 3.7 CCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
78319779 147393 0 None - 0 Mouse 6.9 pEC50 = 6.9 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 629 16 3 10 4.6 N[C@@H](COP(=O)(O)O[C@@H]1CCCO[C@@H]1COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.5b01925
CHEMBL3814092 147393 0 None - 0 Mouse 6.9 pEC50 = 6.9 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 629 16 3 10 4.6 N[C@@H](COP(=O)(O)O[C@@H]1CCCO[C@@H]1COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.5b01925
162656636 187726 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 617 19 3 10 4.5 CCOC[C@H](COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4758243 187726 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 617 19 3 10 4.5 CCOC[C@H](COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
137652635 165670 0 None - 0 Mouse 7.9 pEC50 = 7.9 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 705 18 3 9 7.4 CC(C)(C)c1cccc(-c2ccc(Oc3cccc(COc4ccccc4CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c3)cc2)c1 10.1021/acs.jmedchem.7b00693
CHEMBL4095241 165670 0 None - 0 Mouse 7.9 pEC50 = 7.9 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 705 18 3 9 7.4 CC(C)(C)c1cccc(-c2ccc(Oc3cccc(COc4ccccc4CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c3)cc2)c1 10.1021/acs.jmedchem.7b00693
137652635 165670 0 None - 0 Mouse 7.8 pEC50 = 7.8 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 705 18 3 9 7.4 CC(C)(C)c1cccc(-c2ccc(Oc3cccc(COc4ccccc4CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c3)cc2)c1 10.1021/acs.jmedchem.7b00693
CHEMBL4095241 165670 0 None - 0 Mouse 7.8 pEC50 = 7.8 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 705 18 3 9 7.4 CC(C)(C)c1cccc(-c2ccc(Oc3cccc(COc4ccccc4CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c3)cc2)c1 10.1021/acs.jmedchem.7b00693
137652635 165670 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 705 18 3 9 7.4 CC(C)(C)c1cccc(-c2ccc(Oc3cccc(COc4ccccc4CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c3)cc2)c1 10.1021/acs.jmedchem.7b00693
CHEMBL4095241 165670 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 705 18 3 9 7.4 CC(C)(C)c1cccc(-c2ccc(Oc3cccc(COc4ccccc4CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c3)cc2)c1 10.1021/acs.jmedchem.7b00693
78319779 147393 0 None - 0 Mouse 6.9 pEC50 = 6.9 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 629 16 3 10 4.6 N[C@@H](COP(=O)(O)O[C@@H]1CCCO[C@@H]1COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.5b01925
CHEMBL3814092 147393 0 None - 0 Mouse 6.9 pEC50 = 6.9 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 629 16 3 10 4.6 N[C@@H](COP(=O)(O)O[C@@H]1CCCO[C@@H]1COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.5b01925
52926278 127933 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 495 22 4 8 3.7 CCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
CHEMBL3577144 127933 0 None - 0 Human 5.9 pEC50 = 5.9 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 495 22 4 8 3.7 CCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
137652635 165670 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 705 18 3 9 7.4 CC(C)(C)c1cccc(-c2ccc(Oc3cccc(COc4ccccc4CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c3)cc2)c1 10.1021/acs.jmedchem.7b00693
CHEMBL4095241 165670 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 705 18 3 9 7.4 CC(C)(C)c1cccc(-c2ccc(Oc3cccc(COc4ccccc4CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c3)cc2)c1 10.1021/acs.jmedchem.7b00693
78319779 147393 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 629 16 3 10 4.6 N[C@@H](COP(=O)(O)O[C@@H]1CCCO[C@@H]1COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL3814092 147393 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 629 16 3 10 4.6 N[C@@H](COP(=O)(O)O[C@@H]1CCCO[C@@H]1COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
78319779 147393 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 629 16 3 10 4.6 N[C@@H](COP(=O)(O)O[C@@H]1CCCO[C@@H]1COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL3814092 147393 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 629 16 3 10 4.6 N[C@@H](COP(=O)(O)O[C@@H]1CCCO[C@@H]1COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
122177521 127961 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 617 27 4 9 5.5 CCCCCCCCCCCCCCCOc1cccc(CCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O)c1 10.1021/jm5020082
CHEMBL3577175 127961 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 617 27 4 9 5.5 CCCCCCCCCCCCCCCOc1cccc(CCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O)c1 10.1021/jm5020082
162665010 188901 0 None - 0 Mouse 6.8 pEC50 = 6.8 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 537 25 3 8 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)O[C@H](COC)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4782077 188901 0 None - 0 Mouse 6.8 pEC50 = 6.8 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 537 25 3 8 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)O[C@H](COC)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
122177521 127961 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 617 27 4 9 5.5 CCCCCCCCCCCCCCCOc1cccc(CCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O)c1 10.1021/jm5020082
CHEMBL3577175 127961 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 617 27 4 9 5.5 CCCCCCCCCCCCCCCOc1cccc(CCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O)c1 10.1021/jm5020082
162665010 188901 0 None - 0 Mouse 6.8 pEC50 = 6.8 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 537 25 3 8 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)O[C@H](COC)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4782077 188901 0 None - 0 Mouse 6.8 pEC50 = 6.8 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 537 25 3 8 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)O[C@H](COC)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
122177525 127965 0 None - 0 Mouse 5.8 pEC50 = 5.8 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 545 23 3 8 5.0 CCCCCCCCCCCOc1ccccc1CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL3577179 127965 0 None - 0 Mouse 5.8 pEC50 = 5.8 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 545 23 3 8 5.0 CCCCCCCCCCCOc1ccccc1CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.7b00693
122177525 127965 0 None - 0 Mouse 5.8 pEC50 = 5.8 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 545 23 3 8 5.0 CCCCCCCCCCCOc1ccccc1CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL3577179 127965 0 None - 0 Mouse 5.8 pEC50 = 5.8 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 545 23 3 8 5.0 CCCCCCCCCCCOc1ccccc1CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.7b00693
44475675 203899 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 509 25 3 7 5.7 CCCCCCCCCCCCCCCCCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
CHEMBL567724 203899 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 509 25 3 7 5.7 CCCCCCCCCCCCCCCCCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
137637690 162584 0 None - 0 Mouse 6.8 pEC50 = 6.8 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 607 17 3 9 5.1 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2cccc(Cl)c2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL4059731 162584 0 None - 0 Mouse 6.8 pEC50 = 6.8 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 607 17 3 9 5.1 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2cccc(Cl)c2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
137660207 165980 0 None - 0 Mouse 7.8 pEC50 = 7.8 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 725 19 3 9 7.8 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(-c3ccc(-c4ccccc4)cc3)cc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL4098603 165980 0 None - 0 Mouse 7.8 pEC50 = 7.8 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 725 19 3 9 7.8 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(-c3ccc(-c4ccccc4)cc3)cc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
78319597 188244 0 None - 0 Mouse 6.8 pEC50 = 6.8 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 507 23 3 7 5.5 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@H](C)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4764512 188244 0 None - 0 Mouse 6.8 pEC50 = 6.8 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 507 23 3 7 5.5 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@H](C)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
137637690 162584 0 None - 0 Mouse 6.8 pEC50 = 6.8 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 607 17 3 9 5.1 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2cccc(Cl)c2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL4059731 162584 0 None - 0 Mouse 6.8 pEC50 = 6.8 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 607 17 3 9 5.1 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2cccc(Cl)c2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
44475675 203899 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 509 25 3 7 5.7 CCCCCCCCCCCCCCCCCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
CHEMBL567724 203899 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 509 25 3 7 5.7 CCCCCCCCCCCCCCCCCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
137646507 164576 0 None - 0 Mouse 5.8 pEC50 = 5.8 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 539 19 3 9 3.3 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCCCCOc1ccccc1)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL4083168 164576 0 None - 0 Mouse 5.8 pEC50 = 5.8 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 539 19 3 9 3.3 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCCCCOc1ccccc1)C(=O)O 10.1021/acs.jmedchem.7b00693
78319597 188244 0 None - 0 Mouse 6.8 pEC50 = 6.8 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 507 23 3 7 5.5 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@H](C)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4764512 188244 0 None - 0 Mouse 6.8 pEC50 = 6.8 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 507 23 3 7 5.5 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@H](C)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
137646507 164576 0 None - 0 Mouse 5.8 pEC50 = 5.8 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 539 19 3 9 3.3 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCCCCOc1ccccc1)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL4083168 164576 0 None - 0 Mouse 5.8 pEC50 = 5.8 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 539 19 3 9 3.3 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCCCCOc1ccccc1)C(=O)O 10.1021/acs.jmedchem.7b00693
137646030 164540 0 None - 0 Mouse 6.8 pEC50 = 6.8 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 601 18 3 9 5.0 CCc1ccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.7b00693
CHEMBL4082629 164540 0 None - 0 Mouse 6.8 pEC50 = 6.8 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 601 18 3 9 5.0 CCc1ccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.7b00693
137660207 165980 0 None - 0 Mouse 7.8 pEC50 = 7.8 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 725 19 3 9 7.8 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(-c3ccc(-c4ccccc4)cc3)cc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL4098603 165980 0 None - 0 Mouse 7.8 pEC50 = 7.8 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 725 19 3 9 7.8 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(-c3ccc(-c4ccccc4)cc3)cc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
137645387 164671 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 587 17 3 9 4.8 Cc1ccccc1Oc1cccc(COc2ccccc2CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c1 10.1021/acs.jmedchem.7b00693
CHEMBL4084094 164671 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 587 17 3 9 4.8 Cc1ccccc1Oc1cccc(COc2ccccc2CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c1 10.1021/acs.jmedchem.7b00693
78319779 147393 0 None - 0 Mouse 6.8 pEC50 = 6.8 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 629 16 3 10 4.6 N[C@@H](COP(=O)(O)O[C@@H]1CCCO[C@@H]1COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL3814092 147393 0 None - 0 Mouse 6.8 pEC50 = 6.8 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 629 16 3 10 4.6 N[C@@H](COP(=O)(O)O[C@@H]1CCCO[C@@H]1COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
137646030 164540 0 None - 0 Mouse 6.8 pEC50 = 6.8 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 601 18 3 9 5.0 CCc1ccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.7b00693
CHEMBL4082629 164540 0 None - 0 Mouse 6.8 pEC50 = 6.8 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 601 18 3 9 5.0 CCc1ccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.7b00693
127048989 147425 0 None - 0 Mouse 6.8 pEC50 = 6.8 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 627 16 3 10 4.4 N[C@@H](COP(=O)(O)OC[C@H]1OCC=C[C@H]1OC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.5b01925
CHEMBL3814643 147425 0 None - 0 Mouse 6.8 pEC50 = 6.8 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 627 16 3 10 4.4 N[C@@H](COP(=O)(O)OC[C@H]1OCC=C[C@H]1OC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.5b01925
122177524 127964 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 517 21 3 8 4.2 CCCCCCCCCOc1ccccc1CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
CHEMBL3577178 127964 0 None - 0 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 517 21 3 8 4.2 CCCCCCCCCOc1ccccc1CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
137645387 164671 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 587 17 3 9 4.8 Cc1ccccc1Oc1cccc(COc2ccccc2CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c1 10.1021/acs.jmedchem.7b00693
CHEMBL4084094 164671 0 None - 0 Human 6.7 pEC50 = 6.7 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 587 17 3 9 4.8 Cc1ccccc1Oc1cccc(COc2ccccc2CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c1 10.1021/acs.jmedchem.7b00693
78319779 147393 0 None - 0 Mouse 6.7 pEC50 = 6.7 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 629 16 3 10 4.6 N[C@@H](COP(=O)(O)O[C@@H]1CCCO[C@@H]1COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL3814092 147393 0 None - 0 Mouse 6.7 pEC50 = 6.7 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 629 16 3 10 4.6 N[C@@H](COP(=O)(O)O[C@@H]1CCCO[C@@H]1COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
127048989 147425 0 None - 0 Mouse 6.7 pEC50 = 6.7 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 627 16 3 10 4.4 N[C@@H](COP(=O)(O)OC[C@H]1OCC=C[C@H]1OC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.5b01925
CHEMBL3814643 147425 0 None - 0 Mouse 6.7 pEC50 = 6.7 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 627 16 3 10 4.4 N[C@@H](COP(=O)(O)OC[C@H]1OCC=C[C@H]1OC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.5b01925
122177524 127964 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 517 21 3 8 4.2 CCCCCCCCCOc1ccccc1CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
CHEMBL3577178 127964 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 517 21 3 8 4.2 CCCCCCCCCOc1ccccc1CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
78319778 147388 0 None - 0 Mouse 6.7 pEC50 = 6.7 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 629 16 3 10 4.6 N[C@@H](COP(=O)(O)OC[C@H]1OCCC[C@H]1OC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.5b01925
CHEMBL3813950 147388 0 None - 0 Mouse 6.7 pEC50 = 6.7 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 629 16 3 10 4.6 N[C@@H](COP(=O)(O)OC[C@H]1OCCC[C@H]1OC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.5b01925
78319778 147388 0 None - 0 Mouse 6.7 pEC50 = 6.7 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 629 16 3 10 4.6 N[C@@H](COP(=O)(O)OC[C@H]1OCCC[C@H]1OC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.5b01925
CHEMBL3813950 147388 0 None - 0 Mouse 6.7 pEC50 = 6.7 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 629 16 3 10 4.6 N[C@@H](COP(=O)(O)OC[C@H]1OCCC[C@H]1OC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.5b01925
137652615 165623 0 None - 0 Mouse 5.7 pEC50 = 5.7 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 598 17 3 10 4.3 N#Cc1ccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.7b00693
CHEMBL4094801 165623 0 None - 0 Mouse 5.7 pEC50 = 5.7 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 598 17 3 10 4.3 N#Cc1ccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.7b00693
78319667 187810 0 None - 0 Mouse 8.5 pEC50 = 8.5 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 587 21 3 9 4.8 CCCCCCCCCCCOc1ccccc1CCC(=O)O[C@@H]1COCC[C@H]1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4759297 187810 0 None - 0 Mouse 8.5 pEC50 = 8.5 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 587 21 3 9 4.8 CCCCCCCCCCCOc1ccccc1CCC(=O)O[C@@H]1COCC[C@H]1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
78319667 187810 0 None - 0 Mouse 8.5 pEC50 = 8.5 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 587 21 3 9 4.8 CCCCCCCCCCCOc1ccccc1CCC(=O)O[C@@H]1COCC[C@H]1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4759297 187810 0 None - 0 Mouse 8.5 pEC50 = 8.5 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 587 21 3 9 4.8 CCCCCCCCCCCOc1ccccc1CCC(=O)O[C@@H]1COCC[C@H]1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
137652615 165623 0 None - 0 Mouse 5.7 pEC50 = 5.7 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 598 17 3 10 4.3 N#Cc1ccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.7b00693
CHEMBL4094801 165623 0 None - 0 Mouse 5.7 pEC50 = 5.7 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 598 17 3 10 4.3 N#Cc1ccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.7b00693
145948820 174277 0 None - 0 Mouse 6.7 pEC50 = 6.7 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 563 23 3 8 5.7 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H]1OCCC[C@@H]1OP(=O)(O)OC[C@@H](N)C(=O)O 10.1021/acs.jmedchem.5b01925
CHEMBL4299633 174277 0 None - 0 Mouse 6.7 pEC50 = 6.7 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 563 23 3 8 5.7 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H]1OCCC[C@@H]1OP(=O)(O)OC[C@@H](N)C(=O)O 10.1021/acs.jmedchem.5b01925
137631632 163385 0 None - 0 Mouse 6.7 pEC50 = 6.7 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 629 17 3 9 5.8 CC(C)(C)c1cccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)c1 10.1021/acs.jmedchem.7b00693
CHEMBL4068868 163385 0 None - 0 Mouse 6.7 pEC50 = 6.7 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 629 17 3 9 5.8 CC(C)(C)c1cccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)c1 10.1021/acs.jmedchem.7b00693
145948820 174277 0 None - 0 Mouse 6.7 pEC50 = 6.7 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 563 23 3 8 5.7 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H]1OCCC[C@@H]1OP(=O)(O)OC[C@@H](N)C(=O)O 10.1021/acs.jmedchem.5b01925
CHEMBL4299633 174277 0 None - 0 Mouse 6.7 pEC50 = 6.7 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 563 23 3 8 5.7 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H]1OCCC[C@@H]1OP(=O)(O)OC[C@@H](N)C(=O)O 10.1021/acs.jmedchem.5b01925
137631632 163385 0 None - 0 Mouse 6.7 pEC50 = 6.7 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 629 17 3 9 5.8 CC(C)(C)c1cccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)c1 10.1021/acs.jmedchem.7b00693
CHEMBL4068868 163385 0 None - 0 Mouse 6.7 pEC50 = 6.7 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 629 17 3 9 5.8 CC(C)(C)c1cccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)c1 10.1021/acs.jmedchem.7b00693
162645155 186210 0 None - 0 Mouse 6.7 pEC50 = 6.7 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 587 21 3 9 4.8 CCCCCCCCCCCOc1ccccc1CCC(=O)O[C@@H]1CCOC[C@@H]1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4740368 186210 0 None - 0 Mouse 6.7 pEC50 = 6.7 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 587 21 3 9 4.8 CCCCCCCCCCCOc1ccccc1CCC(=O)O[C@@H]1CCOC[C@@H]1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
162655340 187539 0 None - 0 Mouse 6.7 pEC50 = 6.7 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 559 16 3 9 4.1 N[C@@H](COP(=O)(O)OCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4756147 187539 0 None - 0 Mouse 6.7 pEC50 = 6.7 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 559 16 3 9 4.1 N[C@@H](COP(=O)(O)OCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.0c01126
137640053 163726 0 None - 0 Mouse 6.7 pEC50 = 6.7 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 573 17 3 9 4.5 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL4072692 163726 0 None - 0 Mouse 6.7 pEC50 = 6.7 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 573 17 3 9 4.5 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
162645155 186210 0 None - 0 Mouse 6.7 pEC50 = 6.7 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 587 21 3 9 4.8 CCCCCCCCCCCOc1ccccc1CCC(=O)O[C@@H]1CCOC[C@@H]1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4740368 186210 0 None - 0 Mouse 6.7 pEC50 = 6.7 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 587 21 3 9 4.8 CCCCCCCCCCCOc1ccccc1CCC(=O)O[C@@H]1CCOC[C@@H]1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
162655340 187539 0 None - 0 Mouse 6.7 pEC50 = 6.7 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 559 16 3 9 4.1 N[C@@H](COP(=O)(O)OCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4756147 187539 0 None - 0 Mouse 6.7 pEC50 = 6.7 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 559 16 3 9 4.1 N[C@@H](COP(=O)(O)OCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.0c01126
137640053 163726 0 None - 0 Mouse 6.7 pEC50 = 6.7 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 573 17 3 9 4.5 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL4072692 163726 0 None - 0 Mouse 6.7 pEC50 = 6.7 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 573 17 3 9 4.5 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
137633515 163393 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 587 17 3 9 4.8 Cc1cccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)c1 10.1021/acs.jmedchem.7b00693
CHEMBL4068969 163393 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 587 17 3 9 4.8 Cc1cccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)c1 10.1021/acs.jmedchem.7b00693
78319598 186867 0 None - 0 Mouse 7.6 pEC50 = 7.6 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 507 23 3 7 5.5 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](C)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4748142 186867 0 None - 0 Mouse 7.6 pEC50 = 7.6 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 507 23 3 7 5.5 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](C)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
137633515 163393 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 587 17 3 9 4.8 Cc1cccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)c1 10.1021/acs.jmedchem.7b00693
CHEMBL4068969 163393 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 587 17 3 9 4.8 Cc1cccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)c1 10.1021/acs.jmedchem.7b00693
9547099 67060 2 None - 0 Mouse 6.6 pEC50 = 6.6 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 523 24 4 8 4.5 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL1742484 67060 2 None - 0 Mouse 6.6 pEC50 = 6.6 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 523 24 4 8 4.5 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
122177520 127960 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 617 27 4 9 5.5 CCCCCCCCCCCCCCCOc1ccccc1CCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
CHEMBL3577174 127960 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 617 27 4 9 5.5 CCCCCCCCCCCCCCCOc1ccccc1CCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
9547099 67060 2 None - 0 Mouse 6.6 pEC50 = 6.6 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 523 24 4 8 4.5 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL1742484 67060 2 None - 0 Mouse 6.6 pEC50 = 6.6 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 523 24 4 8 4.5 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
9547099 67060 2 None - 0 Mouse 6.6 pEC50 = 6.6 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 523 24 4 8 4.5 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.5b01925
CHEMBL1742484 67060 2 None - 0 Mouse 6.6 pEC50 = 6.6 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 523 24 4 8 4.5 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.5b01925
78319598 186867 0 None - 0 Mouse 7.6 pEC50 = 7.6 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 507 23 3 7 5.5 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](C)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4748142 186867 0 None - 0 Mouse 7.6 pEC50 = 7.6 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 507 23 3 7 5.5 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](C)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
122177520 127960 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 617 27 4 9 5.5 CCCCCCCCCCCCCCCOc1ccccc1CCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
CHEMBL3577174 127960 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 617 27 4 9 5.5 CCCCCCCCCCCCCCCOc1ccccc1CCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
9547099 67060 2 None - 0 Mouse 6.6 pEC50 = 6.6 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 523 24 4 8 4.5 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.5b01925
CHEMBL1742484 67060 2 None - 0 Mouse 6.6 pEC50 = 6.6 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 523 24 4 8 4.5 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.5b01925
9547099 67060 2 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 523 24 4 8 4.5 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL1742484 67060 2 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 523 24 4 8 4.5 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.7b00693
9547099 67060 2 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 523 24 4 8 4.5 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL1742484 67060 2 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 523 24 4 8 4.5 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.7b00693
162677130 190335 0 None - 0 Mouse 6.6 pEC50 = 6.6 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 507 23 3 7 5.5 CCCCCCCC/C=C\CCCCCCCC(=O)O[C@H](C)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4800263 190335 0 None - 0 Mouse 6.6 pEC50 = 6.6 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 507 23 3 7 5.5 CCCCCCCC/C=C\CCCCCCCC(=O)O[C@H](C)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
162677130 190335 0 None - 0 Mouse 6.6 pEC50 = 6.6 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 507 23 3 7 5.5 CCCCCCCC/C=C\CCCCCCCC(=O)O[C@H](C)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4800263 190335 0 None - 0 Mouse 6.6 pEC50 = 6.6 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 507 23 3 7 5.5 CCCCCCCC/C=C\CCCCCCCC(=O)O[C@H](C)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
137631740 163243 0 None - 0 Mouse 6.6 pEC50 = 6.6 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 603 18 3 10 4.5 COc1ccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.7b00693
CHEMBL4067351 163243 0 None - 0 Mouse 6.6 pEC50 = 6.6 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 603 18 3 10 4.5 COc1ccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.7b00693
137655293 165759 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 587 17 3 9 4.8 Cc1ccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.7b00693
CHEMBL4096239 165759 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 587 17 3 9 4.8 Cc1ccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.7b00693
137631740 163243 0 None - 0 Mouse 6.6 pEC50 = 6.6 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 603 18 3 10 4.5 COc1ccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.7b00693
CHEMBL4067351 163243 0 None - 0 Mouse 6.6 pEC50 = 6.6 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 603 18 3 10 4.5 COc1ccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.7b00693
137635609 162637 0 None - 0 Mouse 5.6 pEC50 = 5.6 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 588 17 4 10 4.1 Nc1ccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.7b00693
CHEMBL4060207 162637 0 None - 0 Mouse 5.6 pEC50 = 5.6 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 588 17 4 10 4.1 Nc1ccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.7b00693
137655293 165759 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 587 17 3 9 4.8 Cc1ccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.7b00693
CHEMBL4096239 165759 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 587 17 3 9 4.8 Cc1ccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.7b00693
137635609 162637 0 None - 0 Mouse 5.6 pEC50 = 5.6 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 588 17 4 10 4.1 Nc1ccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.7b00693
CHEMBL4060207 162637 0 None - 0 Mouse 5.6 pEC50 = 5.6 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 588 17 4 10 4.1 Nc1ccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.7b00693
9547100 127934 3 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 497 23 4 8 3.9 CCCCCCCCCCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
CHEMBL3577145 127934 3 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 497 23 4 8 3.9 CCCCCCCCCCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
9547100 127934 3 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 497 23 4 8 3.9 CCCCCCCCCCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
CHEMBL3577145 127934 3 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 497 23 4 8 3.9 CCCCCCCCCCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
137641921 165170 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 629 17 3 9 5.8 CC(C)(C)c1ccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.7b00693
CHEMBL4089962 165170 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 629 17 3 9 5.8 CC(C)(C)c1ccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.7b00693
118584207 188937 0 None - 0 Mouse 8.5 pEC50 = 8.5 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 551 26 3 8 5.5 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](COCC)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4782438 188937 0 None - 0 Mouse 8.5 pEC50 = 8.5 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 551 26 3 8 5.5 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](COCC)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
118584207 188937 0 None - 0 Mouse 8.5 pEC50 = 8.5 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 551 26 3 8 5.5 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](COCC)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4782438 188937 0 None - 0 Mouse 8.5 pEC50 = 8.5 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 551 26 3 8 5.5 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](COCC)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
137641921 165170 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 629 17 3 9 5.8 CC(C)(C)c1ccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.7b00693
CHEMBL4089962 165170 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 629 17 3 9 5.8 CC(C)(C)c1ccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.7b00693
122177497 127937 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 479 22 3 7 4.7 CCCCCC/C=C\CCCCCCCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
CHEMBL3577149 127937 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 479 22 3 7 4.7 CCCCCC/C=C\CCCCCCCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
122177492 127930 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 535 24 3 7 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)OCC(C)(C)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
CHEMBL3577140 127930 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 535 24 3 7 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)OCC(C)(C)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
162646889 186339 0 None - 0 Mouse 6.5 pEC50 = 6.5 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 521 25 3 7 5.9 CCCCCCCC/C=C\CCCCCCCC(=O)OCCCCOP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4741744 186339 0 None - 0 Mouse 6.5 pEC50 = 6.5 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 521 25 3 7 5.9 CCCCCCCC/C=C\CCCCCCCC(=O)OCCCCOP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
122177497 127937 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 479 22 3 7 4.7 CCCCCC/C=C\CCCCCCCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
CHEMBL3577149 127937 0 None - 0 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 479 22 3 7 4.7 CCCCCC/C=C\CCCCCCCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
122177492 127930 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 535 24 3 7 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)OCC(C)(C)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
CHEMBL3577140 127930 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 535 24 3 7 6.1 CCCCCCCC/C=C\CCCCCCCC(=O)OCC(C)(C)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
162646889 186339 0 None - 0 Mouse 6.5 pEC50 = 6.5 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 521 25 3 7 5.9 CCCCCCCC/C=C\CCCCCCCC(=O)OCCCCOP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4741744 186339 0 None - 0 Mouse 6.5 pEC50 = 6.5 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 521 25 3 7 5.9 CCCCCCCC/C=C\CCCCCCCC(=O)OCCCCOP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
162648818 186600 0 None - 0 Mouse 6.5 pEC50 = 6.5 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 531 22 3 8 4.6 CCCCCCCCCCCOc1ccccc1CCC(=O)OCCOP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4745025 186600 0 None - 0 Mouse 6.5 pEC50 = 6.5 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 531 22 3 8 4.6 CCCCCCCCCCCOc1ccccc1CCC(=O)OCCOP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
162648818 186600 0 None - 0 Mouse 6.5 pEC50 = 6.5 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 531 22 3 8 4.6 CCCCCCCCCCCOc1ccccc1CCC(=O)OCCOP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4745025 186600 0 None - 0 Mouse 6.5 pEC50 = 6.5 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 531 22 3 8 4.6 CCCCCCCCCCCOc1ccccc1CCC(=O)OCCOP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
118555093 187405 0 None - 0 Mouse 6.5 pEC50 = 6.5 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 587 21 3 9 4.8 CCCCCCCCCCCOc1ccccc1CCC(=O)O[C@H]1COCC[C@H]1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4754776 187405 0 None - 0 Mouse 6.5 pEC50 = 6.5 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 587 21 3 9 4.8 CCCCCCCCCCCOc1ccccc1CCC(=O)O[C@H]1COCC[C@H]1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
78319776 147376 0 None - 0 Mouse 6.5 pEC50 = 6.5 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 629 16 3 10 4.6 N[C@@H](COP(=O)(O)O[C@H]1CCCO[C@@H]1COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.5b01925
CHEMBL3813773 147376 0 None - 0 Mouse 6.5 pEC50 = 6.5 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 629 16 3 10 4.6 N[C@@H](COP(=O)(O)O[C@H]1CCCO[C@@H]1COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.5b01925
118555093 187405 0 None - 0 Mouse 6.5 pEC50 = 6.5 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 587 21 3 9 4.8 CCCCCCCCCCCOc1ccccc1CCC(=O)O[C@H]1COCC[C@H]1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4754776 187405 0 None - 0 Mouse 6.5 pEC50 = 6.5 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 587 21 3 9 4.8 CCCCCCCCCCCOc1ccccc1CCC(=O)O[C@H]1COCC[C@H]1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
78319776 147376 0 None - 0 Mouse 6.5 pEC50 = 6.5 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 629 16 3 10 4.6 N[C@@H](COP(=O)(O)O[C@H]1CCCO[C@@H]1COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.5b01925
CHEMBL3813773 147376 0 None - 0 Mouse 6.5 pEC50 = 6.5 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 629 16 3 10 4.6 N[C@@H](COP(=O)(O)O[C@H]1CCCO[C@@H]1COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.5b01925
127051443 147452 0 None - 0 Mouse 7.5 pEC50 = 7.5 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 643 16 3 10 4.9 Cc1ccc(Oc2cccc(COc3ccccc3CCC(=O)OC[C@H]3OCCC[C@H]3OP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.5b01925
CHEMBL3815069 147452 0 None - 0 Mouse 7.5 pEC50 = 7.5 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 643 16 3 10 4.9 Cc1ccc(Oc2cccc(COc3ccccc3CCC(=O)OC[C@H]3OCCC[C@H]3OP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.5b01925
127051443 147452 0 None - 0 Mouse 7.4 pEC50 = 7.4 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 643 16 3 10 4.9 Cc1ccc(Oc2cccc(COc3ccccc3CCC(=O)OC[C@H]3OCCC[C@H]3OP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.5b01925
CHEMBL3815069 147452 0 None - 0 Mouse 7.4 pEC50 = 7.4 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 643 16 3 10 4.9 Cc1ccc(Oc2cccc(COc3ccccc3CCC(=O)OC[C@H]3OCCC[C@H]3OP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.5b01925
127053035 147417 0 None - 0 Mouse 7.4 pEC50 = 7.4 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 663 16 3 10 5.3 N[C@@H](COP(=O)(O)O[C@@H]1CCCO[C@@H]1COC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(Cl)cc2)c1)C(=O)O 10.1021/acs.jmedchem.5b01925
CHEMBL3814525 147417 0 None - 0 Mouse 7.4 pEC50 = 7.4 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 663 16 3 10 5.3 N[C@@H](COP(=O)(O)O[C@@H]1CCCO[C@@H]1COC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(Cl)cc2)c1)C(=O)O 10.1021/acs.jmedchem.5b01925
127053035 147417 0 None - 0 Mouse 7.4 pEC50 = 7.4 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 663 16 3 10 5.3 N[C@@H](COP(=O)(O)O[C@@H]1CCCO[C@@H]1COC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(Cl)cc2)c1)C(=O)O 10.1021/acs.jmedchem.5b01925
CHEMBL3814525 147417 0 None - 0 Mouse 7.4 pEC50 = 7.4 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 663 16 3 10 5.3 N[C@@H](COP(=O)(O)O[C@@H]1CCCO[C@@H]1COC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(Cl)cc2)c1)C(=O)O 10.1021/acs.jmedchem.5b01925
137655293 165759 0 None - 0 Mouse 7.4 pEC50 = 7.4 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 587 17 3 9 4.8 Cc1ccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.7b00693
CHEMBL4096239 165759 0 None - 0 Mouse 7.4 pEC50 = 7.4 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 587 17 3 9 4.8 Cc1ccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.7b00693
137655293 165759 0 None - 0 Mouse 7.4 pEC50 = 7.4 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 587 17 3 9 4.8 Cc1ccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.7b00693
CHEMBL4096239 165759 0 None - 0 Mouse 7.4 pEC50 = 7.4 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 587 17 3 9 4.8 Cc1ccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.7b00693
137660207 165980 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 725 19 3 9 7.8 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(-c3ccc(-c4ccccc4)cc3)cc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL4098603 165980 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 725 19 3 9 7.8 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(-c3ccc(-c4ccccc4)cc3)cc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
137660207 165980 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 725 19 3 9 7.8 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(-c3ccc(-c4ccccc4)cc3)cc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL4098603 165980 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 725 19 3 9 7.8 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(-c3ccc(-c4ccccc4)cc3)cc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
122177490 127929 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 523 24 4 8 4.5 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
CHEMBL3577138 127929 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 523 24 4 8 4.5 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
122177490 127929 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 523 24 4 8 4.5 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
CHEMBL3577138 127929 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 523 24 4 8 4.5 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
9547099 67060 2 None - 0 Mouse 6.4 pEC50 = 6.4 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 523 24 4 8 4.5 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL1742484 67060 2 None - 0 Mouse 6.4 pEC50 = 6.4 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 523 24 4 8 4.5 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.7b00693
9547099 67060 2 None - 0 Mouse 6.4 pEC50 = 6.4 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 523 24 4 8 4.5 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL1742484 67060 2 None - 0 Mouse 6.4 pEC50 = 6.4 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 523 24 4 8 4.5 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.7b00693
137644526 165259 0 None - 0 Mouse 7.4 pEC50 = 7.4 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 649 18 3 9 6.1 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(-c3ccccc3)cc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL4090880 165259 0 None - 0 Mouse 7.4 pEC50 = 7.4 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 649 18 3 9 6.1 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(-c3ccccc3)cc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
137644526 165259 0 None - 0 Mouse 7.3 pEC50 = 7.3 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 649 18 3 9 6.1 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(-c3ccccc3)cc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL4090880 165259 0 None - 0 Mouse 7.3 pEC50 = 7.3 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 649 18 3 9 6.1 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(-c3ccccc3)cc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
122177517 127957 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 561 23 4 9 4.0 CCCCCCCCCCCOc1ccccc1CCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
CHEMBL3577171 127957 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 561 23 4 9 4.0 CCCCCCCCCCCOc1ccccc1CCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
122177517 127957 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 561 23 4 9 4.0 CCCCCCCCCCCOc1ccccc1CCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
CHEMBL3577171 127957 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 561 23 4 9 4.0 CCCCCCCCCCCOc1ccccc1CCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
78319746 147395 0 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 627 16 3 10 4.4 N[C@@H](COP(=O)(O)O[C@H]1C=CCO[C@@H]1COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.5b01925
CHEMBL3814147 147395 0 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 627 16 3 10 4.4 N[C@@H](COP(=O)(O)O[C@H]1C=CCO[C@@H]1COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.5b01925
162674211 189911 0 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 535 26 3 7 6.3 CCCCCCCC/C=C\CCCCCCCC(=O)OCCCCCOP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4795101 189911 0 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 535 26 3 7 6.3 CCCCCCCC/C=C\CCCCCCCC(=O)OCCCCCOP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
78319746 147395 0 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 627 16 3 10 4.4 N[C@@H](COP(=O)(O)O[C@H]1C=CCO[C@@H]1COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.5b01925
CHEMBL3814147 147395 0 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 627 16 3 10 4.4 N[C@@H](COP(=O)(O)O[C@H]1C=CCO[C@@H]1COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.5b01925
162674211 189911 0 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 535 26 3 7 6.3 CCCCCCCC/C=C\CCCCCCCC(=O)OCCCCCOP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4795101 189911 0 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 535 26 3 7 6.3 CCCCCCCC/C=C\CCCCCCCC(=O)OCCCCCOP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
137639110 163630 0 None - 0 Mouse 7.3 pEC50 = 7.3 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 749 24 3 10 8.1 CCCCCCOc1ccc(-c2ccc(Oc3cccc(COc4ccccc4CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c3)cc2)cc1 10.1021/acs.jmedchem.7b00693
CHEMBL4071570 163630 0 None - 0 Mouse 7.3 pEC50 = 7.3 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 749 24 3 10 8.1 CCCCCCOc1ccc(-c2ccc(Oc3cccc(COc4ccccc4CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c3)cc2)cc1 10.1021/acs.jmedchem.7b00693
137639110 163630 0 None - 0 Mouse 7.3 pEC50 = 7.3 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 749 24 3 10 8.1 CCCCCCOc1ccc(-c2ccc(Oc3cccc(COc4ccccc4CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c3)cc2)cc1 10.1021/acs.jmedchem.7b00693
CHEMBL4071570 163630 0 None - 0 Mouse 7.3 pEC50 = 7.3 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 749 24 3 10 8.1 CCCCCCOc1ccc(-c2ccc(Oc3cccc(COc4ccccc4CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c3)cc2)cc1 10.1021/acs.jmedchem.7b00693
162656636 187726 0 None - 0 Mouse 8.3 pEC50 = 8.3 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 617 19 3 10 4.5 CCOC[C@H](COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4758243 187726 0 None - 0 Mouse 8.3 pEC50 = 8.3 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 617 19 3 10 4.5 CCOC[C@H](COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
162656636 187726 0 None - 0 Mouse 8.3 pEC50 = 8.3 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 617 19 3 10 4.5 CCOC[C@H](COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4758243 187726 0 None - 0 Mouse 8.3 pEC50 = 8.3 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 617 19 3 10 4.5 CCOC[C@H](COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
78319666 187848 0 None - 0 Mouse 8.3 pEC50 = 8.3 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 603 18 3 10 4.1 COC[C@H](COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4759762 187848 0 None - 0 Mouse 8.3 pEC50 = 8.3 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 603 18 3 10 4.1 COC[C@H](COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
78319666 187848 0 None - 0 Mouse 8.2 pEC50 = 8.2 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 603 18 3 10 4.1 COC[C@H](COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4759762 187848 0 None - 0 Mouse 8.2 pEC50 = 8.2 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 603 18 3 10 4.1 COC[C@H](COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
78319710 147373 0 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 599 22 3 9 4.9 CCCCCCCCCCCOc1ccccc1CCC(=O)OC[C@H]1OCC=C[C@H]1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.5b01925
CHEMBL3813751 147373 0 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 599 22 3 9 4.9 CCCCCCCCCCCOc1ccccc1CCC(=O)OC[C@H]1OCC=C[C@H]1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.5b01925
78319710 147373 0 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 599 22 3 9 4.9 CCCCCCCCCCCOc1ccccc1CCC(=O)OC[C@H]1OCC=C[C@H]1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.5b01925
CHEMBL3813751 147373 0 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 599 22 3 9 4.9 CCCCCCCCCCCOc1ccccc1CCC(=O)OC[C@H]1OCC=C[C@H]1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.5b01925
71495077 127928 0 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 507 24 3 7 5.5 CCCCCCCC/C=C\CCCCCCCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL3577137 127928 0 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 507 24 3 7 5.5 CCCCCCCC/C=C\CCCCCCCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
71495077 127928 0 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 507 24 3 7 5.5 CCCCCCCC/C=C\CCCCCCCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL3577137 127928 0 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 507 24 3 7 5.5 CCCCCCCC/C=C\CCCCCCCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
9547099 67060 2 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 523 24 4 8 4.5 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
CHEMBL1742484 67060 2 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 523 24 4 8 4.5 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
137633515 163393 0 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 587 17 3 9 4.8 Cc1cccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)c1 10.1021/acs.jmedchem.7b00693
CHEMBL4068969 163393 0 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 587 17 3 9 4.8 Cc1cccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)c1 10.1021/acs.jmedchem.7b00693
127048654 147379 0 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 561 23 3 8 5.4 CCCCCCCC/C=C\CCCCCCCC(=O)O[C@@H]1C=CCO[C@@H]1COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.5b01925
CHEMBL3813812 147379 0 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 561 23 3 8 5.4 CCCCCCCC/C=C\CCCCCCCC(=O)O[C@@H]1C=CCO[C@@H]1COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.5b01925
9547099 67060 2 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 523 24 4 8 4.5 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
CHEMBL1742484 67060 2 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 523 24 4 8 4.5 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
137633515 163393 0 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 587 17 3 9 4.8 Cc1cccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)c1 10.1021/acs.jmedchem.7b00693
CHEMBL4068969 163393 0 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 587 17 3 9 4.8 Cc1cccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)c1 10.1021/acs.jmedchem.7b00693
127048654 147379 0 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 561 23 3 8 5.4 CCCCCCCC/C=C\CCCCCCCC(=O)O[C@@H]1C=CCO[C@@H]1COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.5b01925
CHEMBL3813812 147379 0 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 561 23 3 8 5.4 CCCCCCCC/C=C\CCCCCCCC(=O)O[C@@H]1C=CCO[C@@H]1COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.5b01925
162643129 188453 0 None - 0 Mouse 8.2 pEC50 = 8.2 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 565 27 3 8 5.9 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](COCCC)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4776455 188453 0 None - 0 Mouse 8.2 pEC50 = 8.2 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 565 27 3 8 5.9 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](COCCC)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
162643129 188453 0 None - 0 Mouse 8.2 pEC50 = 8.2 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 565 27 3 8 5.9 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](COCCC)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4776455 188453 0 None - 0 Mouse 8.2 pEC50 = 8.2 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 565 27 3 8 5.9 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](COCCC)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
162648728 186659 0 None - 0 Mouse 8.2 pEC50 = 8.2 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 573 16 3 9 4.5 C[C@H](COP(=O)(O)OC[C@H](N)C(=O)O)OC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1 10.1021/acs.jmedchem.0c01126
CHEMBL4745697 186659 0 None - 0 Mouse 8.2 pEC50 = 8.2 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 573 16 3 9 4.5 C[C@H](COP(=O)(O)OC[C@H](N)C(=O)O)OC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1 10.1021/acs.jmedchem.0c01126
162648728 186659 0 None - 0 Mouse 8.2 pEC50 = 8.2 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 573 16 3 9 4.5 C[C@H](COP(=O)(O)OC[C@H](N)C(=O)O)OC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1 10.1021/acs.jmedchem.0c01126
CHEMBL4745697 186659 0 None - 0 Mouse 8.2 pEC50 = 8.2 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 573 16 3 9 4.5 C[C@H](COP(=O)(O)OC[C@H](N)C(=O)O)OC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1 10.1021/acs.jmedchem.0c01126
78319744 147402 0 None - 0 Mouse 6.2 pEC50 = 6.2 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 627 16 3 10 4.4 N[C@@H](COP(=O)(O)O[C@@H]1C=CCO[C@@H]1COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.5b01925
CHEMBL3814235 147402 0 None - 0 Mouse 6.2 pEC50 = 6.2 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 627 16 3 10 4.4 N[C@@H](COP(=O)(O)O[C@@H]1C=CCO[C@@H]1COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.5b01925
78319744 147402 0 None - 0 Mouse 6.2 pEC50 = 6.2 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 627 16 3 10 4.4 N[C@@H](COP(=O)(O)O[C@@H]1C=CCO[C@@H]1COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.5b01925
CHEMBL3814235 147402 0 None - 0 Mouse 6.2 pEC50 = 6.2 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 627 16 3 10 4.4 N[C@@H](COP(=O)(O)O[C@@H]1C=CCO[C@@H]1COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.5b01925
78319629 187014 0 None - 0 Mouse 6.2 pEC50 = 6.2 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 537 25 3 8 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@H](COC)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4750036 187014 0 None - 0 Mouse 6.2 pEC50 = 6.2 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 537 25 3 8 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@H](COC)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
78319629 187014 0 None - 0 Mouse 6.2 pEC50 = 6.2 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 537 25 3 8 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@H](COC)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4750036 187014 0 None - 0 Mouse 6.2 pEC50 = 6.2 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 537 25 3 8 5.1 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@H](COC)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
118555084 190002 0 None - 0 Mouse 7.2 pEC50 = 7.2 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 587 21 3 9 4.8 CCCCCCCCCCCOc1ccccc1CCC(=O)O[C@@H]1COCC[C@@H]1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4796110 190002 0 None - 0 Mouse 7.2 pEC50 = 7.2 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 587 21 3 9 4.8 CCCCCCCCCCCOc1ccccc1CCC(=O)O[C@@H]1COCC[C@@H]1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
118555084 190002 0 None - 0 Mouse 7.2 pEC50 = 7.2 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 587 21 3 9 4.8 CCCCCCCCCCCOc1ccccc1CCC(=O)O[C@@H]1COCC[C@@H]1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4796110 190002 0 None - 0 Mouse 7.2 pEC50 = 7.2 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 587 21 3 9 4.8 CCCCCCCCCCCOc1ccccc1CCC(=O)O[C@@H]1COCC[C@@H]1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
118555087 147390 0 None - 0 Mouse 6.2 pEC50 = 6.2 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 601 22 3 9 5.2 CCCCCCCCCCCOc1ccccc1CCC(=O)OC[C@H]1OCCC[C@@H]1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.5b01925
CHEMBL3814009 147390 0 None - 0 Mouse 6.2 pEC50 = 6.2 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 601 22 3 9 5.2 CCCCCCCCCCCOc1ccccc1CCC(=O)OC[C@H]1OCCC[C@@H]1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.5b01925
137645387 164671 0 None - 0 Mouse 6.2 pEC50 = 6.2 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 587 17 3 9 4.8 Cc1ccccc1Oc1cccc(COc2ccccc2CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c1 10.1021/acs.jmedchem.7b00693
CHEMBL4084094 164671 0 None - 0 Mouse 6.2 pEC50 = 6.2 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 587 17 3 9 4.8 Cc1ccccc1Oc1cccc(COc2ccccc2CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c1 10.1021/acs.jmedchem.7b00693
118555087 147390 0 None - 0 Mouse 6.2 pEC50 = 6.2 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 601 22 3 9 5.2 CCCCCCCCCCCOc1ccccc1CCC(=O)OC[C@H]1OCCC[C@@H]1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.5b01925
CHEMBL3814009 147390 0 None - 0 Mouse 6.2 pEC50 = 6.2 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 601 22 3 9 5.2 CCCCCCCCCCCOc1ccccc1CCC(=O)OC[C@H]1OCCC[C@@H]1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.5b01925
137645387 164671 0 None - 0 Mouse 6.2 pEC50 = 6.2 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 587 17 3 9 4.8 Cc1ccccc1Oc1cccc(COc2ccccc2CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c1 10.1021/acs.jmedchem.7b00693
CHEMBL4084094 164671 0 None - 0 Mouse 6.2 pEC50 = 6.2 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 587 17 3 9 4.8 Cc1ccccc1Oc1cccc(COc2ccccc2CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c1 10.1021/acs.jmedchem.7b00693
137636212 162864 0 None - 0 Mouse 8.1 pEC50 = 8.1 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 705 18 3 9 7.4 CC(C)(C)c1ccc(-c2ccc(Oc3cccc(COc4ccccc4CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c3)cc2)cc1 10.1021/acs.jmedchem.7b00693
CHEMBL4062945 162864 0 None - 0 Mouse 8.1 pEC50 = 8.1 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 705 18 3 9 7.4 CC(C)(C)c1ccc(-c2ccc(Oc3cccc(COc4ccccc4CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c3)cc2)cc1 10.1021/acs.jmedchem.7b00693
137636212 162864 0 None - 0 Mouse 8.1 pEC50 = 8.1 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 705 18 3 9 7.4 CC(C)(C)c1ccc(-c2ccc(Oc3cccc(COc4ccccc4CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c3)cc2)cc1 10.1021/acs.jmedchem.7b00693
CHEMBL4062945 162864 0 None - 0 Mouse 8.1 pEC50 = 8.1 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 705 18 3 9 7.4 CC(C)(C)c1ccc(-c2ccc(Oc3cccc(COc4ccccc4CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c3)cc2)cc1 10.1021/acs.jmedchem.7b00693
122177499 127939 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 453 21 3 7 4.2 CCCCCCCCCCCCCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
CHEMBL3577151 127939 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 453 21 3 7 4.2 CCCCCCCCCCCCCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
127051792 147454 0 None - 0 Mouse 6.2 pEC50 = 6.2 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 593 22 3 8 6.2 CCCCCCCCCCCOc1ccccc1CCC(=O)OCc1ccccc1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.5b01925
CHEMBL3815090 147454 0 None - 0 Mouse 6.2 pEC50 = 6.2 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 593 22 3 8 6.2 CCCCCCCCCCCOc1ccccc1CCC(=O)OCc1ccccc1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.5b01925
122177499 127939 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 453 21 3 7 4.2 CCCCCCCCCCCCCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
CHEMBL3577151 127939 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 453 21 3 7 4.2 CCCCCCCCCCCCCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
127051792 147454 0 None - 0 Mouse 6.2 pEC50 = 6.2 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 593 22 3 8 6.2 CCCCCCCCCCCOc1ccccc1CCC(=O)OCc1ccccc1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.5b01925
CHEMBL3815090 147454 0 None - 0 Mouse 6.2 pEC50 = 6.2 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 593 22 3 8 6.2 CCCCCCCCCCCOc1ccccc1CCC(=O)OCc1ccccc1OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.5b01925
127051772 147438 0 None - 0 Mouse 7.1 pEC50 = 7.1 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 643 16 3 10 4.9 Cc1ccc(Oc2cccc(COc3ccccc3CCC(=O)O[C@@H]3CCCO[C@@H]3COP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.5b01925
CHEMBL3814818 147438 0 None - 0 Mouse 7.1 pEC50 = 7.1 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 643 16 3 10 4.9 Cc1ccc(Oc2cccc(COc3ccccc3CCC(=O)O[C@@H]3CCCO[C@@H]3COP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.5b01925
127051772 147438 0 None - 0 Mouse 7.1 pEC50 = 7.1 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 643 16 3 10 4.9 Cc1ccc(Oc2cccc(COc3ccccc3CCC(=O)O[C@@H]3CCCO[C@@H]3COP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.5b01925
CHEMBL3814818 147438 0 None - 0 Mouse 7.1 pEC50 = 7.1 Binding
Agonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assayAgonist activity at mouse GPR34 expressed in HEK293A cells cotransfected with chimeric Galphaq/il after 1.5 hrs by alkaline phosphatase tagged-TGFalpha shedding assay
ChEMBL 643 16 3 10 4.9 Cc1ccc(Oc2cccc(COc3ccccc3CCC(=O)O[C@@H]3CCCO[C@@H]3COP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.5b01925
137644526 165259 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 649 18 3 9 6.1 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(-c3ccccc3)cc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL4090880 165259 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 649 18 3 9 6.1 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(-c3ccccc3)cc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
137631421 163291 0 None - 0 Mouse 7.1 pEC50 = 7.1 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 663 18 3 9 6.4 Cc1ccccc1-c1ccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.7b00693
CHEMBL4067822 163291 0 None - 0 Mouse 7.1 pEC50 = 7.1 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 663 18 3 9 6.4 Cc1ccccc1-c1ccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.7b00693
137644526 165259 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 649 18 3 9 6.1 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(-c3ccccc3)cc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL4090880 165259 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 649 18 3 9 6.1 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(-c3ccccc3)cc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
137631421 163291 0 None - 0 Mouse 7.1 pEC50 = 7.1 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 663 18 3 9 6.4 Cc1ccccc1-c1ccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.7b00693
CHEMBL4067822 163291 0 None - 0 Mouse 7.1 pEC50 = 7.1 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 663 18 3 9 6.4 Cc1ccccc1-c1ccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.7b00693
137660359 166293 0 None - 0 Mouse 6.1 pEC50 = 6.1 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 579 17 3 9 4.4 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(OC2CCCCC2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL4102082 166293 0 None - 0 Mouse 6.1 pEC50 = 6.1 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 579 17 3 9 4.4 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(OC2CCCCC2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
137660359 166293 0 None - 0 Mouse 6.1 pEC50 = 6.1 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 579 17 3 9 4.4 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(OC2CCCCC2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL4102082 166293 0 None - 0 Mouse 6.1 pEC50 = 6.1 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 579 17 3 9 4.4 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(OC2CCCCC2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
137643805 165218 0 None - 0 Mouse 7.1 pEC50 = 7.1 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 651 17 3 9 5.2 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(Br)cc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL4090455 165218 0 None - 0 Mouse 7.1 pEC50 = 7.1 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 651 17 3 9 5.2 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(Br)cc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
137643805 165218 0 None - 0 Mouse 7.1 pEC50 = 7.1 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 651 17 3 9 5.2 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(Br)cc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL4090455 165218 0 None - 0 Mouse 7.1 pEC50 = 7.1 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 651 17 3 9 5.2 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccc(Br)cc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
52926276 127936 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 441 19 4 8 2.4 CCCCCCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
CHEMBL3577147 127936 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 441 19 4 8 2.4 CCCCCCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
52926276 127936 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 441 19 4 8 2.4 CCCCCCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
CHEMBL3577147 127936 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 441 19 4 8 2.4 CCCCCCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
118584208 186770 0 None - 0 Mouse 6.1 pEC50 = 6.1 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 613 27 3 8 6.7 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](COCc1ccccc1)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4746971 186770 0 None - 0 Mouse 6.1 pEC50 = 6.1 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 613 27 3 8 6.7 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](COCc1ccccc1)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
118584208 186770 0 None - 0 Mouse 6.1 pEC50 = 6.1 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 613 27 3 8 6.7 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](COCc1ccccc1)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4746971 186770 0 None - 0 Mouse 6.1 pEC50 = 6.1 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 613 27 3 8 6.7 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](COCc1ccccc1)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
76900162 187864 0 None - 0 Mouse 8.1 pEC50 = 8.1 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 573 16 3 9 4.5 C[C@H](COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4759998 187864 0 None - 0 Mouse 8.1 pEC50 = 8.1 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 573 16 3 9 4.5 C[C@H](COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
76900162 187864 0 None - 0 Mouse 8.0 pEC50 = 8.0 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 573 16 3 9 4.5 C[C@H](COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
CHEMBL4759998 187864 0 None - 0 Mouse 8.0 pEC50 = 8.0 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysisAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr by p-NPP substrate based microplate reader analysis
ChEMBL 573 16 3 9 4.5 C[C@H](COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)OP(=O)(O)OC[C@H](N)C(=O)O 10.1021/acs.jmedchem.0c01126
137640053 163726 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 573 17 3 9 4.5 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL4072692 163726 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 573 17 3 9 4.5 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
137641921 165170 0 None - 0 Mouse 6.1 pEC50 = 6.1 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 629 17 3 9 5.8 CC(C)(C)c1ccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.7b00693
CHEMBL4089962 165170 0 None - 0 Mouse 6.1 pEC50 = 6.1 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 629 17 3 9 5.8 CC(C)(C)c1ccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.7b00693
137641921 165170 0 None - 0 Mouse 6.0 pEC50 = 6.0 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 629 17 3 9 5.8 CC(C)(C)c1ccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.7b00693
CHEMBL4089962 165170 0 None - 0 Mouse 6.0 pEC50 = 6.0 Binding
Agonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hrAgonist activity at mouse GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of ectodomain shedding of membrane bound AP-TGFalpha after 1 hr
ChEMBL 629 17 3 9 5.8 CC(C)(C)c1ccc(Oc2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 10.1021/acs.jmedchem.7b00693
122177516 127956 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 533 21 4 9 3.2 CCCCCCCCCOc1ccccc1CCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
CHEMBL3577170 127956 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 533 21 4 9 3.2 CCCCCCCCCOc1ccccc1CCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
122177516 127956 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 533 21 4 9 3.2 CCCCCCCCCOc1ccccc1CCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
CHEMBL3577170 127956 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 533 21 4 9 3.2 CCCCCCCCCOc1ccccc1CCC(=O)OC[C@@H](O)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
122177528 127968 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 563 23 3 8 5.0 CCCCCCCCCCCOc1ccccc1CCC(=O)OC[C@@H](F)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
CHEMBL3577182 127968 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 563 23 3 8 5.0 CCCCCCCCCCCOc1ccccc1CCC(=O)OC[C@@H](F)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
122177528 127968 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 563 23 3 8 5.0 CCCCCCCCCCCOc1ccccc1CCC(=O)OC[C@@H](F)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
CHEMBL3577182 127968 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assayAgonist activity at GPR34 (unknown origin) transfected in HEK293A cells after 1 hr by TGFalpha shedding assay
ChEMBL 563 23 3 8 5.0 CCCCCCCCCCCOc1ccccc1CCC(=O)OC[C@@H](F)COP(=O)(O)OC[C@H](N)C(=O)O 10.1021/jm5020082
137640053 163726 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 573 17 3 9 4.5 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693
CHEMBL4072692 163726 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hrAgonist activity at human GPR34 expressed in HEK293 cells co-transfected with AP-TGFalpha/chimeric Galphaq/i1 assessed as induction of AP-TGFalpha release after 1 hr
ChEMBL 573 17 3 9 4.5 N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.7b00693