Ligand source activities (1 row/activity)
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
| 172441879 | 194941 | None | 0 | Mouse | Functional | pEC50 | = | 5.8 | 5.8 | -602 | 2 | Agonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release by TGFalpha shedding assayAgonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release by TGFalpha shedding assay |
ChEMBL | 544 | 23 | 3 | 8 | 4.4 | CCCCCCCCCCCOc1ccccc1CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(N)=O | 10.1016/j.ejmech.2023.115271 | ||
| CHEMBL5393782 | 194941 | None | 0 | Mouse | Functional | pEC50 | = | 5.8 | 5.8 | -602 | 2 | Agonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release by TGFalpha shedding assayAgonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release by TGFalpha shedding assay |
ChEMBL | 544 | 23 | 3 | 8 | 4.4 | CCCCCCCCCCCOc1ccccc1CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(N)=O | 10.1016/j.ejmech.2023.115271 | ||
| 172441879 | 194941 | None | 0 | Mouse | Functional | pEC50 | = | 5.8 | 5.8 | -602 | 2 | Agonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release by TGFalpha shedding assayAgonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release by TGFalpha shedding assay |
ChEMBL | 544 | 23 | 3 | 8 | 4.4 | CCCCCCCCCCCOc1ccccc1CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(N)=O | 10.1016/j.ejmech.2023.115271 | ||
| CHEMBL5393782 | 194941 | None | 0 | Mouse | Functional | pEC50 | = | 5.8 | 5.8 | -602 | 2 | Agonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release by TGFalpha shedding assayAgonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release by TGFalpha shedding assay |
ChEMBL | 544 | 23 | 3 | 8 | 4.4 | CCCCCCCCCCCOc1ccccc1CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(N)=O | 10.1016/j.ejmech.2023.115271 | ||
| 172447361 | 195786 | None | 0 | Mouse | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | Agonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release by TGFalpha shedding assayAgonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release by TGFalpha shedding assay |
ChEMBL | 629 | 16 | 3 | 10 | 4.6 | N[C@@H](COP(=O)(O)OC1CCCO[C@@H]1COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O | 10.1016/j.ejmech.2023.115271 | ||
| CHEMBL5410755 | 195786 | None | 0 | Mouse | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | Agonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release by TGFalpha shedding assayAgonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release by TGFalpha shedding assay |
ChEMBL | 629 | 16 | 3 | 10 | 4.6 | N[C@@H](COP(=O)(O)OC1CCCO[C@@H]1COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O | 10.1016/j.ejmech.2023.115271 | ||
| 172447361 | 195786 | None | 0 | Mouse | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | Agonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release by TGFalpha shedding assayAgonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release by TGFalpha shedding assay |
ChEMBL | 629 | 16 | 3 | 10 | 4.6 | N[C@@H](COP(=O)(O)OC1CCCO[C@@H]1COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O | 10.1016/j.ejmech.2023.115271 | ||
| CHEMBL5410755 | 195786 | None | 0 | Mouse | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | Agonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release by TGFalpha shedding assayAgonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release by TGFalpha shedding assay |
ChEMBL | 629 | 16 | 3 | 10 | 4.6 | N[C@@H](COP(=O)(O)OC1CCCO[C@@H]1COC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O | 10.1016/j.ejmech.2023.115271 | ||
| 137640053 | 157039 | None | 0 | Mouse | Functional | pEC50 | = | 6.7 | 6.7 | -2 | 3 | Agonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release by TGFalpha shedding assayAgonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release by TGFalpha shedding assay |
ChEMBL | 573 | 17 | 3 | 9 | 4.5 | N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O | 10.1016/j.ejmech.2023.115271 | ||
| CHEMBL4072692 | 157039 | None | 0 | Mouse | Functional | pEC50 | = | 6.7 | 6.7 | -2 | 3 | Agonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release by TGFalpha shedding assayAgonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release by TGFalpha shedding assay |
ChEMBL | 573 | 17 | 3 | 9 | 4.5 | N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O | 10.1016/j.ejmech.2023.115271 | ||
| 137640053 | 157039 | None | 0 | Mouse | Functional | pEC50 | = | 6.7 | 6.7 | -2 | 3 | Agonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release by TGFalpha shedding assayAgonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release by TGFalpha shedding assay |
ChEMBL | 573 | 17 | 3 | 9 | 4.5 | N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O | 10.1016/j.ejmech.2023.115271 | ||
| CHEMBL4072692 | 157039 | None | 0 | Mouse | Functional | pEC50 | = | 6.7 | 6.7 | -2 | 3 | Agonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release by TGFalpha shedding assayAgonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release by TGFalpha shedding assay |
ChEMBL | 573 | 17 | 3 | 9 | 4.5 | N[C@@H](COP(=O)(O)OCCCOC(=O)CCc1ccccc1OCc1cccc(Oc2ccccc2)c1)C(=O)O | 10.1016/j.ejmech.2023.115271 | ||
| 9547099 | 60306 | None | 2 | Mouse | Functional | pEC50 | = | 6.5 | 6.5 | -17 | 6 | Agonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release by TGFalpha shedding assayAgonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release 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 | 10.1016/j.ejmech.2023.115271 | ||
| CHEMBL1742484 | 60306 | None | 2 | Mouse | Functional | pEC50 | = | 6.5 | 6.5 | -17 | 6 | Agonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release by TGFalpha shedding assayAgonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release 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 | 10.1016/j.ejmech.2023.115271 | ||
| 9547099 | 60306 | None | 2 | Mouse | Functional | pEC50 | = | 6.5 | 6.5 | -17 | 6 | Agonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release by TGFalpha shedding assayAgonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release 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 | 10.1016/j.ejmech.2023.115271 | ||
| CHEMBL1742484 | 60306 | None | 2 | Mouse | Functional | pEC50 | = | 6.5 | 6.5 | -17 | 6 | Agonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release by TGFalpha shedding assayAgonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release 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 | 10.1016/j.ejmech.2023.115271 | ||
| 172446827 | 195181 | None | 0 | Mouse | Functional | pEC50 | = | 6.0 | 6.0 | -27 | 2 | Agonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release by TGFalpha shedding assayAgonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release by TGFalpha shedding assay |
ChEMBL | 613 | 16 | 3 | 8 | 5.6 | CC(C)(C)c1ccc(-c2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 | 10.1016/j.ejmech.2023.115271 | ||
| CHEMBL5398282 | 195181 | None | 0 | Mouse | Functional | pEC50 | = | 6.0 | 6.0 | -27 | 2 | Agonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release by TGFalpha shedding assayAgonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release by TGFalpha shedding assay |
ChEMBL | 613 | 16 | 3 | 8 | 5.6 | CC(C)(C)c1ccc(-c2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 | 10.1016/j.ejmech.2023.115271 | ||
| 172446827 | 195181 | None | 0 | Mouse | Functional | pEC50 | = | 6.0 | 6.0 | -27 | 2 | Agonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release by TGFalpha shedding assayAgonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release by TGFalpha shedding assay |
ChEMBL | 613 | 16 | 3 | 8 | 5.6 | CC(C)(C)c1ccc(-c2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 | 10.1016/j.ejmech.2023.115271 | ||
| CHEMBL5398282 | 195181 | None | 0 | Mouse | Functional | pEC50 | = | 6.0 | 6.0 | -27 | 2 | Agonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release by TGFalpha shedding assayAgonist activity at mouse LPS1/GPR34 transfected in HEK293-A cells co-transfected with AP-TGFalpha assessed as AP-TGFalpha release by TGFalpha shedding assay |
ChEMBL | 613 | 16 | 3 | 8 | 5.6 | CC(C)(C)c1ccc(-c2cccc(COc3ccccc3CCC(=O)OCCCOP(=O)(O)OC[C@H](N)C(=O)O)c2)cc1 | 10.1016/j.ejmech.2023.115271 | ||
| 4064 | 2435 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | -3 | 3 | 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 | 2435 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | -3 | 3 | 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 | 2435 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | -3 | 3 | 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 | 2435 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | -3 | 3 | 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 | 2435 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | -3 | 3 | 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 | 2435 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | -3 | 3 | 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 | 2435 | None | 0 | Mouse | Functional | pEC50 | = | 7.3 | 7.3 | 1 | 3 | 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 | 2435 | None | 0 | Mouse | Functional | pEC50 | = | 7.3 | 7.3 | 1 | 3 | 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 | 2435 | None | 0 | Mouse | Functional | pEC50 | = | 7.3 | 7.3 | 1 | 3 | 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 | 4114 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | - | 1 | 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 | 4114 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | - | 1 | 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 | ||
Showing 1 to 31 of 31 entries
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
| 78319665 | 180599 | None | 0 | Human | Binding | pEC50 | = | 9.1 | 9.1 | - | 0 | 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 | 180599 | None | 0 | Human | Binding | pEC50 | = | 9.1 | 9.1 | - | 0 | 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 | 180599 | None | 0 | Human | Binding | pEC50 | = | 9.1 | 9.1 | - | 0 | 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 | 180599 | None | 0 | Human | Binding | pEC50 | = | 9.1 | 9.1 | - | 0 | 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 | 180599 | None | 0 | Mouse | Binding | pEC50 | = | 9.1 | 9.1 | - | 0 | 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 | 180599 | None | 0 | Mouse | Binding | pEC50 | = | 9.1 | 9.1 | - | 0 | 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 | 180599 | None | 0 | Mouse | Binding | pEC50 | = | 9.1 | 9.1 | - | 0 | 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 | 180599 | None | 0 | Mouse | Binding | pEC50 | = | 9.1 | 9.1 | - | 0 | 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 | 181597 | None | 0 | Mouse | Binding | pEC50 | = | 8.0 | 8.0 | - | 0 | 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 | 181597 | None | 0 | Mouse | Binding | pEC50 | = | 8.0 | 8.0 | - | 0 | 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 | 159479 | None | 0 | Mouse | Binding | pEC50 | = | 7 | 7.0 | - | 0 | 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 | 159479 | None | 0 | Mouse | Binding | pEC50 | = | 7 | 7.0 | - | 0 | 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 | 167598 | None | 0 | Mouse | Binding | pEC50 | = | 7 | 7.0 | - | 0 | 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 | 167598 | None | 0 | Mouse | Binding | pEC50 | = | 7 | 7.0 | - | 0 | 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 | 159479 | None | 0 | Mouse | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | 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 | 159479 | None | 0 | Mouse | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | 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 | 159247 | None | 0 | Mouse | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | 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 | 159247 | None | 0 | Mouse | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | 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 | 140742 | None | 0 | Mouse | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | 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 | 140742 | None | 0 | Mouse | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | 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 | 181597 | None | 0 | Mouse | Binding | pEC50 | = | 8.0 | 8.0 | - | 0 | 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 | 181597 | None | 0 | Mouse | Binding | pEC50 | = | 8.0 | 8.0 | - | 0 | 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 | 182453 | None | 0 | Mouse | Binding | pEC50 | = | 7.9 | 7.9 | - | 0 | 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 | 182453 | None | 0 | Mouse | Binding | pEC50 | = | 7.9 | 7.9 | - | 0 | 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 | 159247 | None | 0 | Mouse | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | 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 | 159247 | None | 0 | Mouse | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | 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 | 140742 | None | 0 | Mouse | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | 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 | 140742 | None | 0 | Mouse | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | 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 | 156899 | None | 0 | Mouse | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | 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 | 156899 | None | 0 | Mouse | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | 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 | 156133 | None | 0 | Mouse | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | 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 | 156133 | None | 0 | Mouse | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | 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 | 140769 | None | 0 | Mouse | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | 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 | 140769 | None | 0 | Mouse | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | 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 | 182453 | None | 0 | Mouse | Binding | pEC50 | = | 7.9 | 7.9 | - | 0 | 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 | 182453 | None | 0 | Mouse | Binding | pEC50 | = | 7.9 | 7.9 | - | 0 | 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 | 156133 | None | 0 | Mouse | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | 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 | 156133 | None | 0 | Mouse | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | 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 | 156899 | None | 0 | Mouse | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | 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 | 156899 | None | 0 | Mouse | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | 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 | 140769 | None | 0 | Mouse | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | 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 | 140769 | None | 0 | Mouse | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | 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 | 156048 | None | 0 | Mouse | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | 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 | 156048 | None | 0 | Mouse | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | 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 | 157770 | None | 0 | Mouse | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | 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 | 157770 | None | 0 | Mouse | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | 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 | 156048 | None | 0 | Mouse | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | 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 | 156048 | None | 0 | Mouse | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | 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 | 157770 | None | 0 | Mouse | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | 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 | 157770 | None | 0 | Mouse | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | 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 | ||
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