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
| |
| 2733504 | 1434 | None | 13 | Human | Functional | pEC50 | = | 6 | 6.0 | -3 | 3 | Agonist activity at FLAG/GFP-tagged GPR3 (unknown origin)-mediated cAMP signaling in HEK293 cells using d2-cAMP as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by HTRF assayAgonist activity at FLAG/GFP-tagged GPR3 (unknown origin)-mediated cAMP signaling in HEK293 cells using d2-cAMP as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by HTRF assay |
ChEMBL | 314 | 0 | 0 | 0 | -3.2 | c1ccc2c(c1)[I+]c1c2cccc1.[Cl-] | 10.1021/acs.jmedchem.3c01707 | ||
| 7802 | 1434 | None | 13 | Human | Functional | pEC50 | = | 6 | 6.0 | -3 | 3 | Agonist activity at FLAG/GFP-tagged GPR3 (unknown origin)-mediated cAMP signaling in HEK293 cells using d2-cAMP as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by HTRF assayAgonist activity at FLAG/GFP-tagged GPR3 (unknown origin)-mediated cAMP signaling in HEK293 cells using d2-cAMP as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by HTRF assay |
ChEMBL | 314 | 0 | 0 | 0 | -3.2 | c1ccc2c(c1)[I+]c1c2cccc1.[Cl-] | 10.1021/acs.jmedchem.3c01707 | ||
| CHEMBL365739 | 1434 | None | 13 | Human | Functional | pEC50 | = | 6 | 6.0 | -3 | 3 | Agonist activity at FLAG/GFP-tagged GPR3 (unknown origin)-mediated cAMP signaling in HEK293 cells using d2-cAMP as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by HTRF assayAgonist activity at FLAG/GFP-tagged GPR3 (unknown origin)-mediated cAMP signaling in HEK293 cells using d2-cAMP as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by HTRF assay |
ChEMBL | 314 | 0 | 0 | 0 | -3.2 | c1ccc2c(c1)[I+]c1c2cccc1.[Cl-] | 10.1021/acs.jmedchem.3c01707 | ||
| CHEMBL397686 | 1434 | None | 13 | Human | Functional | pEC50 | = | 6 | 6.0 | -3 | 3 | Agonist activity at FLAG/GFP-tagged GPR3 (unknown origin)-mediated cAMP signaling in HEK293 cells using d2-cAMP as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by HTRF assayAgonist activity at FLAG/GFP-tagged GPR3 (unknown origin)-mediated cAMP signaling in HEK293 cells using d2-cAMP as substrate preincubated for 30 mins followed by substrate addition measured after 60 mins by HTRF assay |
ChEMBL | 314 | 0 | 0 | 0 | -3.2 | c1ccc2c(c1)[I+]c1c2cccc1.[Cl-] | 10.1021/acs.jmedchem.3c01707 | ||
| 172462474 | 196829 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 377 | 2 | 0 | 1 | 0.7 | FC(F)(F)COc1ccc2c(c1)[I+]c1ccccc1-2 | 10.1016/j.bmcl.2023.129427 | ||
| CHEMBL5432982 | 196829 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 377 | 2 | 0 | 1 | 0.7 | FC(F)(F)COc1ccc2c(c1)[I+]c1ccccc1-2 | 10.1016/j.bmcl.2023.129427 | ||
| 134817096 | 167633 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 297 | 0 | 0 | 0 | -0.1 | Fc1ccc2c(c1)[I+]c1ccccc1-2 | 10.1016/j.bmcl.2023.129427 | ||
| CHEMBL4300174 | 167633 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 297 | 0 | 0 | 0 | -0.1 | Fc1ccc2c(c1)[I+]c1ccccc1-2 | 10.1016/j.bmcl.2023.129427 | ||
| 4086473 | 196335 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 324 | 1 | 0 | 2 | -0.3 | O=[N+]([O-])c1ccc2c(c1)[I+]c1ccccc1-2 | 10.1016/j.bmcl.2023.129427 | ||
| CHEMBL5421637 | 196335 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 324 | 1 | 0 | 2 | -0.3 | O=[N+]([O-])c1ccc2c(c1)[I+]c1ccccc1-2 | 10.1016/j.bmcl.2023.129427 | ||
| 172453881 | 196008 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 381 | 1 | 0 | 1 | 0.8 | Fc1ccc2c(c1)[I+]c1cc(OC(F)(F)F)ccc1-2 | 10.1016/j.bmcl.2023.129427 | ||
| CHEMBL5415054 | 196008 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 381 | 1 | 0 | 1 | 0.8 | Fc1ccc2c(c1)[I+]c1cc(OC(F)(F)F)ccc1-2 | 10.1016/j.bmcl.2023.129427 | ||
| 172462319 | 196735 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 363 | 5 | 0 | 0 | 1.9 | CCCCCCc1ccc2c(c1)[I+]c1ccccc1-2 | 10.1016/j.bmcl.2023.129427 | ||
| CHEMBL5431176 | 196735 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 363 | 5 | 0 | 0 | 1.9 | CCCCCCc1ccc2c(c1)[I+]c1ccccc1-2 | 10.1016/j.bmcl.2023.129427 | ||
| 71543612 | 167846 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 309 | 1 | 0 | 1 | -0.2 | COc1ccc2c(c1)[I+]c1ccccc1-2 | 10.1016/j.bmcl.2023.129427 | ||
| CHEMBL4302860 | 167846 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 309 | 1 | 0 | 1 | -0.2 | COc1ccc2c(c1)[I+]c1ccccc1-2 | 10.1016/j.bmcl.2023.129427 | ||
| 172445328 | 195073 | None | 0 | Human | Functional | pEC50 | = | 4.7 | 4.7 | - | 1 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 359 | 0 | 0 | 2 | 0.1 | FC1(F)Oc2cc3c(cc2O1)-c1ccccc1[I+]3 | 10.1016/j.bmcl.2023.129427 | ||
| CHEMBL5396263 | 195073 | None | 0 | Human | Functional | pEC50 | = | 4.7 | 4.7 | - | 1 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 359 | 0 | 0 | 2 | 0.1 | FC1(F)Oc2cc3c(cc2O1)-c1ccccc1[I+]3 | 10.1016/j.bmcl.2023.129427 | ||
| 265040 | 194995 | None | 13 | Human | Functional | pEC50 | = | 4.7 | 4.7 | - | 1 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 209 | 1 | 0 | 1 | 3.3 | CN(C)C1c2ccccc2-c2ccccc21 | 10.1016/j.bmcl.2023.129427 | ||
| CHEMBL5394629 | 194995 | None | 13 | Human | Functional | pEC50 | = | 4.7 | 4.7 | - | 1 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 209 | 1 | 0 | 1 | 3.3 | CN(C)C1c2ccccc2-c2ccccc21 | 10.1016/j.bmcl.2023.129427 | ||
| 172460988 | 196521 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | - | 1 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 399 | 1 | 0 | 1 | 1.0 | Fc1cc2c(cc1F)-c1ccc(OC(F)(F)F)cc1[I+]2 | 10.1016/j.bmcl.2023.129427 | ||
| CHEMBL5425788 | 196521 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | - | 1 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 399 | 1 | 0 | 1 | 1.0 | Fc1cc2c(cc1F)-c1ccc(OC(F)(F)F)cc1[I+]2 | 10.1016/j.bmcl.2023.129427 | ||
| 169450677 | 195267 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | - | 1 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 363 | 1 | 0 | 1 | 0.7 | FC(F)(F)Oc1ccc2c(c1)[I+]c1ccccc1-2 | 10.1016/j.bmcl.2023.129427 | ||
| CHEMBL5399736 | 195267 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | - | 1 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 363 | 1 | 0 | 1 | 0.7 | FC(F)(F)Oc1ccc2c(c1)[I+]c1ccccc1-2 | 10.1016/j.bmcl.2023.129427 | ||
| 172464243 | 196781 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | - | 1 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 447 | 2 | 0 | 2 | 1.6 | FC(F)(F)Oc1ccc2c(c1)[I+]c1cc(OC(F)(F)F)ccc1-2 | 10.1016/j.bmcl.2023.129427 | ||
| CHEMBL5432166 | 196781 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | - | 1 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 447 | 2 | 0 | 2 | 1.6 | FC(F)(F)Oc1ccc2c(c1)[I+]c1cc(OC(F)(F)F)ccc1-2 | 10.1016/j.bmcl.2023.129427 | ||
| 9190 | 57430 | None | 48 | Human | Functional | pEC50 | = | 4.5 | 4.5 | - | 1 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 180 | 0 | 0 | 2 | 2.8 | c1ccc2c(c1)nnc1ccccc12 | 10.1016/j.bmcl.2023.129427 | ||
| CHEMBL1652414 | 57430 | None | 48 | Human | Functional | pEC50 | = | 4.5 | 4.5 | - | 1 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 180 | 0 | 0 | 2 | 2.8 | c1ccc2c(c1)nnc1ccccc12 | 10.1016/j.bmcl.2023.129427 | ||
| 172468235 | 196887 | None | 0 | Human | Functional | pEC50 | = | 5.5 | 5.5 | - | 1 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 311 | 0 | 0 | 0 | 0.2 | Cc1cc2c(cc1F)-c1ccccc1[I+]2 | 10.1016/j.bmcl.2023.129427 | ||
| CHEMBL5434234 | 196887 | None | 0 | Human | Functional | pEC50 | = | 5.5 | 5.5 | - | 1 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 311 | 0 | 0 | 0 | 0.2 | Cc1cc2c(cc1F)-c1ccccc1[I+]2 | 10.1016/j.bmcl.2023.129427 | ||
| 2733504 | 1434 | None | 13 | Human | Functional | pEC50 | = | 5.4 | 5.4 | -3 | 3 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 314 | 0 | 0 | 0 | -3.2 | c1ccc2c(c1)[I+]c1c2cccc1.[Cl-] | 10.1016/j.bmcl.2023.129427 | ||
| 7802 | 1434 | None | 13 | Human | Functional | pEC50 | = | 5.4 | 5.4 | -3 | 3 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 314 | 0 | 0 | 0 | -3.2 | c1ccc2c(c1)[I+]c1c2cccc1.[Cl-] | 10.1016/j.bmcl.2023.129427 | ||
| CHEMBL365739 | 1434 | None | 13 | Human | Functional | pEC50 | = | 5.4 | 5.4 | -3 | 3 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 314 | 0 | 0 | 0 | -3.2 | c1ccc2c(c1)[I+]c1c2cccc1.[Cl-] | 10.1016/j.bmcl.2023.129427 | ||
| CHEMBL397686 | 1434 | None | 13 | Human | Functional | pEC50 | = | 5.4 | 5.4 | -3 | 3 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 314 | 0 | 0 | 0 | -3.2 | c1ccc2c(c1)[I+]c1c2cccc1.[Cl-] | 10.1016/j.bmcl.2023.129427 | ||
| 15142 | 67792 | None | 58 | Human | Functional | pEC50 | = | 4.4 | 4.4 | - | 1 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 181 | 0 | 0 | 1 | 3.3 | Cn1c2ccccc2c2ccccc21 | 10.1016/j.bmcl.2023.129427 | ||
| CHEMBL1908211 | 67792 | None | 58 | Human | Functional | pEC50 | = | 4.4 | 4.4 | - | 1 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 181 | 0 | 0 | 1 | 3.3 | Cn1c2ccccc2c2ccccc21 | 10.1016/j.bmcl.2023.129427 | ||
| 1853 | 173344 | None | 66 | Human | Functional | pEC50 | = | 4.4 | 4.4 | - | 1 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 195 | 0 | 1 | 1 | 2.7 | O=c1[nH]c2ccccc2c2ccccc12 | 10.1016/j.bmcl.2023.129427 | ||
| CHEMBL45245 | 173344 | None | 66 | Human | Functional | pEC50 | = | 4.4 | 4.4 | - | 1 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 195 | 0 | 1 | 1 | 2.7 | O=c1[nH]c2ccccc2c2ccccc12 | 10.1016/j.bmcl.2023.129427 | ||
| 172449189 | 195690 | None | 0 | Human | Functional | pEC50 | = | 6.3 | 6.3 | - | 1 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 377 | 1 | 0 | 1 | 1.0 | Cc1ccc2c(c1)[I+]c1cc(OC(F)(F)F)ccc1-2 | 10.1016/j.bmcl.2023.129427 | ||
| CHEMBL5409202 | 195690 | None | 0 | Human | Functional | pEC50 | = | 6.3 | 6.3 | - | 1 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 377 | 1 | 0 | 1 | 1.0 | Cc1ccc2c(c1)[I+]c1cc(OC(F)(F)F)ccc1-2 | 10.1016/j.bmcl.2023.129427 | ||
| 13908 | 195535 | None | 54 | Human | Functional | pEC50 | = | 5.3 | 5.3 | - | 1 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 216 | 0 | 0 | 2 | 2.5 | O=S1(=O)c2ccccc2-c2ccccc21 | 10.1016/j.bmcl.2023.129427 | ||
| CHEMBL5405489 | 195535 | None | 54 | Human | Functional | pEC50 | = | 5.3 | 5.3 | - | 1 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 216 | 0 | 0 | 2 | 2.5 | O=S1(=O)c2ccccc2-c2ccccc21 | 10.1016/j.bmcl.2023.129427 | ||
| 2733504 | 1434 | None | 13 | Human | Functional | pEC50 | = | 5.3 | 5.3 | -3 | 3 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 314 | 0 | 0 | 0 | -3.2 | c1ccc2c(c1)[I+]c1c2cccc1.[Cl-] | 10.1016/j.bmcl.2023.129427 | ||
| 7802 | 1434 | None | 13 | Human | Functional | pEC50 | = | 5.3 | 5.3 | -3 | 3 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 314 | 0 | 0 | 0 | -3.2 | c1ccc2c(c1)[I+]c1c2cccc1.[Cl-] | 10.1016/j.bmcl.2023.129427 | ||
| CHEMBL365739 | 1434 | None | 13 | Human | Functional | pEC50 | = | 5.3 | 5.3 | -3 | 3 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 314 | 0 | 0 | 0 | -3.2 | c1ccc2c(c1)[I+]c1c2cccc1.[Cl-] | 10.1016/j.bmcl.2023.129427 | ||
| CHEMBL397686 | 1434 | None | 13 | Human | Functional | pEC50 | = | 5.3 | 5.3 | -3 | 3 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 314 | 0 | 0 | 0 | -3.2 | c1ccc2c(c1)[I+]c1c2cccc1.[Cl-] | 10.1016/j.bmcl.2023.129427 | ||
| 242966 | 59667 | None | 2 | Human | Functional | pEC50 | = | 4.2 | 4.2 | - | 1 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 209 | 0 | 0 | 1 | 3.9 | CC1c2ccccc2-c2ccccc2N1C | 10.1016/j.bmcl.2023.129427 | ||
| CHEMBL1721150 | 59667 | None | 2 | Human | Functional | pEC50 | = | 4.2 | 4.2 | - | 1 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 209 | 0 | 0 | 1 | 3.9 | CC1c2ccccc2-c2ccccc2N1C | 10.1016/j.bmcl.2023.129427 | ||
| 85743780 | 167687 | None | 0 | Human | Functional | pEC50 | = | 5.2 | 5.2 | - | 1 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 293 | 0 | 0 | 0 | 0.1 | Cc1ccc2c(c1)[I+]c1ccccc1-2 | 10.1016/j.bmcl.2023.129427 | ||
| CHEMBL4173205 | 167687 | None | 0 | Human | Functional | pEC50 | = | 5.2 | 5.2 | - | 1 | Agonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human GPR3 expressed in HEK293 cells assessed as increase in cAMP accumulation incubated for 30 mins by HTRF assay |
ChEMBL | 293 | 0 | 0 | 0 | 0.1 | Cc1ccc2c(c1)[I+]c1ccccc1-2 | 10.1016/j.bmcl.2023.129427 | ||
Showing 1 to 50 of 77 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
| |
| 172447166 | 195003 | None | 0 | Human | Binding | pEC50 | = | 5.0 | 5.0 | - | 0 | Total binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assayTotal binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assay |
ChEMBL | 920 | 19 | 2 | 12 | 9.6 | CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccc(OCCCCCCNC(=O)c3ccc(-c4c5ccc(N(C)C)cc5[o+]c5cc(N(C)C)ccc45)c(C(=O)[O-])c3)cc2)nc2ncnn12 | 10.1021/acs.jmedchem.3c01707 | ||
| CHEMBL5394725 | 195003 | None | 0 | Human | Binding | pEC50 | = | 5.0 | 5.0 | - | 0 | Total binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assayTotal binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assay |
ChEMBL | 920 | 19 | 2 | 12 | 9.6 | CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccc(OCCCCCCNC(=O)c3ccc(-c4c5ccc(N(C)C)cc5[o+]c5cc(N(C)C)ccc45)c(C(=O)[O-])c3)cc2)nc2ncnn12 | 10.1021/acs.jmedchem.3c01707 | ||
| 172452129 | 195773 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | -7 | 2 | Modulation of N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate at 1 uM measured for 3 hrs in presence of DPI by NanoBRET assayModulation of N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate at 1 uM measured for 3 hrs in presence of DPI by NanoBRET assay |
ChEMBL | 920 | 19 | 2 | 12 | 9.6 | CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccccc2OCCCCCCNC(=O)c2ccc(-c3c4ccc(N(C)C)cc4[o+]c4cc(N(C)C)ccc34)c(C(=O)[O-])c2)nc2ncnn12 | 10.1021/acs.jmedchem.3c01707 | ||
| CHEMBL5410506 | 195773 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | -7 | 2 | Modulation of N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate at 1 uM measured for 3 hrs in presence of DPI by NanoBRET assayModulation of N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate at 1 uM measured for 3 hrs in presence of DPI by NanoBRET assay |
ChEMBL | 920 | 19 | 2 | 12 | 9.6 | CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccccc2OCCCCCCNC(=O)c2ccc(-c3c4ccc(N(C)C)cc4[o+]c4cc(N(C)C)ccc34)c(C(=O)[O-])c2)nc2ncnn12 | 10.1021/acs.jmedchem.3c01707 | ||
| 172442960 | 195543 | None | 0 | Human | Binding | pEC50 | = | 5.5 | 5.5 | - | 0 | Total binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assayTotal binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assay |
ChEMBL | 996 | 24 | 2 | 15 | 8.0 | CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccccc2OCCOCCOCCOCCNC(=O)c2ccc(-c3c4ccc(N(C)C)cc4[o+]c4cc(N(C)C)ccc34)c(C(=O)[O-])c2)nc2ncnn12 | 10.1021/acs.jmedchem.3c01707 | ||
| CHEMBL5405597 | 195543 | None | 0 | Human | Binding | pEC50 | = | 5.5 | 5.5 | - | 0 | Total binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assayTotal binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assay |
ChEMBL | 996 | 24 | 2 | 15 | 8.0 | CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccccc2OCCOCCOCCOCCNC(=O)c2ccc(-c3c4ccc(N(C)C)cc4[o+]c4cc(N(C)C)ccc34)c(C(=O)[O-])c2)nc2ncnn12 | 10.1021/acs.jmedchem.3c01707 | ||
| 172445374 | 195171 | None | 0 | Human | Binding | pEC50 | = | 5.4 | 5.4 | - | 0 | Total binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assayTotal binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assay |
ChEMBL | 1084 | 30 | 2 | 17 | 8.1 | CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccccc2OCCOCCOCCOCCOCCOCCNC(=O)c2ccc(-c3c4ccc(N(C)C)cc4[o+]c4cc(N(C)C)ccc34)c(C(=O)[O-])c2)nc2ncnn12 | 10.1021/acs.jmedchem.3c01707 | ||
| CHEMBL5398023 | 195171 | None | 0 | Human | Binding | pEC50 | = | 5.4 | 5.4 | - | 0 | Total binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assayTotal binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assay |
ChEMBL | 1084 | 30 | 2 | 17 | 8.1 | CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccccc2OCCOCCOCCOCCOCCOCCNC(=O)c2ccc(-c3c4ccc(N(C)C)cc4[o+]c4cc(N(C)C)ccc34)c(C(=O)[O-])c2)nc2ncnn12 | 10.1021/acs.jmedchem.3c01707 | ||
| 172458638 | 196423 | None | 0 | Human | Binding | pEC50 | = | 5.4 | 5.4 | - | 0 | Total binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assayTotal binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assay |
ChEMBL | 920 | 19 | 2 | 12 | 9.6 | CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2cccc(OCCCCCCNC(=O)c3ccc(-c4c5ccc(N(C)C)cc5[o+]c5cc(N(C)C)ccc45)c(C(=O)[O-])c3)c2)nc2ncnn12 | 10.1021/acs.jmedchem.3c01707 | ||
| CHEMBL5423734 | 196423 | None | 0 | Human | Binding | pEC50 | = | 5.4 | 5.4 | - | 0 | Total binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assayTotal binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assay |
ChEMBL | 920 | 19 | 2 | 12 | 9.6 | CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2cccc(OCCCCCCNC(=O)c3ccc(-c4c5ccc(N(C)C)cc5[o+]c5cc(N(C)C)ccc45)c(C(=O)[O-])c3)c2)nc2ncnn12 | 10.1021/acs.jmedchem.3c01707 | ||
| 172452129 | 195773 | None | 0 | Human | Binding | pEC50 | = | 6.1 | 6.1 | -7 | 2 | Total binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assayTotal binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assay |
ChEMBL | 920 | 19 | 2 | 12 | 9.6 | CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccccc2OCCCCCCNC(=O)c2ccc(-c3c4ccc(N(C)C)cc4[o+]c4cc(N(C)C)ccc34)c(C(=O)[O-])c2)nc2ncnn12 | 10.1021/acs.jmedchem.3c01707 | ||
| CHEMBL5410506 | 195773 | None | 0 | Human | Binding | pEC50 | = | 6.1 | 6.1 | -7 | 2 | Total binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assayTotal binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assay |
ChEMBL | 920 | 19 | 2 | 12 | 9.6 | CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccccc2OCCCCCCNC(=O)c2ccc(-c3c4ccc(N(C)C)cc4[o+]c4cc(N(C)C)ccc34)c(C(=O)[O-])c2)nc2ncnn12 | 10.1021/acs.jmedchem.3c01707 | ||
| 172452129 | 195773 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | -7 | 2 | Competitive total binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate at 1 uM measured for 3 hrs in presence of AF64394 by NanoBRET assayCompetitive total binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate at 1 uM measured for 3 hrs in presence of AF64394 by NanoBRET assay |
ChEMBL | 920 | 19 | 2 | 12 | 9.6 | CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccccc2OCCCCCCNC(=O)c2ccc(-c3c4ccc(N(C)C)cc4[o+]c4cc(N(C)C)ccc34)c(C(=O)[O-])c2)nc2ncnn12 | 10.1021/acs.jmedchem.3c01707 | ||
| CHEMBL5410506 | 195773 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | -7 | 2 | Competitive total binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate at 1 uM measured for 3 hrs in presence of AF64394 by NanoBRET assayCompetitive total binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate at 1 uM measured for 3 hrs in presence of AF64394 by NanoBRET assay |
ChEMBL | 920 | 19 | 2 | 12 | 9.6 | CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccccc2OCCCCCCNC(=O)c2ccc(-c3c4ccc(N(C)C)cc4[o+]c4cc(N(C)C)ccc34)c(C(=O)[O-])c2)nc2ncnn12 | 10.1021/acs.jmedchem.3c01707 | ||
| 172452129 | 195773 | None | 0 | Human | Binding | pKd | = | 7.0 | 7.0 | -7 | 2 | Binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using vivazine as substrate measured for 180 mins by time-course saturation based NanoBRET assayBinding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using vivazine as substrate measured for 180 mins by time-course saturation based NanoBRET assay |
ChEMBL | 920 | 19 | 2 | 12 | 9.6 | CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccccc2OCCCCCCNC(=O)c2ccc(-c3c4ccc(N(C)C)cc4[o+]c4cc(N(C)C)ccc34)c(C(=O)[O-])c2)nc2ncnn12 | 10.1021/acs.jmedchem.3c01707 | ||
| CHEMBL5410506 | 195773 | None | 0 | Human | Binding | pKd | = | 7.0 | 7.0 | -7 | 2 | Binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using vivazine as substrate measured for 180 mins by time-course saturation based NanoBRET assayBinding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using vivazine as substrate measured for 180 mins by time-course saturation based NanoBRET assay |
ChEMBL | 920 | 19 | 2 | 12 | 9.6 | CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccccc2OCCCCCCNC(=O)c2ccc(-c3c4ccc(N(C)C)cc4[o+]c4cc(N(C)C)ccc34)c(C(=O)[O-])c2)nc2ncnn12 | 10.1021/acs.jmedchem.3c01707 | ||
| 172452129 | 195773 | None | 0 | Human | Binding | pKd | = | 6.5 | 6.5 | -7 | 2 | Specific binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assaySpecific binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assay |
ChEMBL | 920 | 19 | 2 | 12 | 9.6 | CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccccc2OCCCCCCNC(=O)c2ccc(-c3c4ccc(N(C)C)cc4[o+]c4cc(N(C)C)ccc34)c(C(=O)[O-])c2)nc2ncnn12 | 10.1021/acs.jmedchem.3c01707 | ||
| CHEMBL5410506 | 195773 | None | 0 | Human | Binding | pKd | = | 6.5 | 6.5 | -7 | 2 | Specific binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assaySpecific binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate measured for 3 hrs by NanoBRET assay |
ChEMBL | 920 | 19 | 2 | 12 | 9.6 | CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccccc2OCCCCCCNC(=O)c2ccc(-c3c4ccc(N(C)C)cc4[o+]c4cc(N(C)C)ccc34)c(C(=O)[O-])c2)nc2ncnn12 | 10.1021/acs.jmedchem.3c01707 | ||
| 172452129 | 195773 | None | 0 | Human | Binding | pKi | = | 6.5 | 6.5 | -7 | 2 | Competitive total binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate at 1 uM measured for 3 hrs in presence of AF64394 by NanoBRET assayCompetitive total binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate at 1 uM measured for 3 hrs in presence of AF64394 by NanoBRET assay |
ChEMBL | 920 | 19 | 2 | 12 | 9.6 | CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccccc2OCCCCCCNC(=O)c2ccc(-c3c4ccc(N(C)C)cc4[o+]c4cc(N(C)C)ccc34)c(C(=O)[O-])c2)nc2ncnn12 | 10.1021/acs.jmedchem.3c01707 | ||
| CHEMBL5410506 | 195773 | None | 0 | Human | Binding | pKi | = | 6.5 | 6.5 | -7 | 2 | Competitive total binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate at 1 uM measured for 3 hrs in presence of AF64394 by NanoBRET assayCompetitive total binding affinity to N-terminal 3xHA/Nluc-tagged full-length wild-type human GPR3 expressed in HEK293A cells using furimazine as substrate at 1 uM measured for 3 hrs in presence of AF64394 by NanoBRET assay |
ChEMBL | 920 | 19 | 2 | 12 | 9.6 | CC(C)Oc1cc(Cl)ccc1CNc1cc(-c2ccccc2OCCCCCCNC(=O)c2ccc(-c3c4ccc(N(C)C)cc4[o+]c4cc(N(C)C)ccc34)c(C(=O)[O-])c2)nc2ncnn12 | 10.1021/acs.jmedchem.3c01707 | ||
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