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
| |
| 118727607 | 117570 | None | 0 | Human | Functional | pEC50 | = | 9.2 | 9.2 | - | 1 | Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay |
ChEMBL | 410 | 6 | 1 | 2 | 5.8 | NC1(CN(C(=O)[C@@H]2C[C@H]2c2ccccc2)c2ccc(-c3ccccc3)cc2)CCCC1 | 10.1016/j.bmcl.2015.02.038 | ||
| CHEMBL3400199 | 117570 | None | 0 | Human | Functional | pEC50 | = | 9.2 | 9.2 | - | 1 | Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay |
ChEMBL | 410 | 6 | 1 | 2 | 5.8 | NC1(CN(C(=O)[C@@H]2C[C@H]2c2ccccc2)c2ccc(-c3ccccc3)cc2)CCCC1 | 10.1016/j.bmcl.2015.02.038 | ||
| 118730169 | 118122 | None | 0 | Human | Functional | pEC50 | = | 9.2 | 9.2 | - | 1 | Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay |
ChEMBL | 438 | 7 | 1 | 2 | 6.4 | N[C@H](CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1)C1CCCCC1 | 10.1016/j.bmcl.2015.02.038 | ||
| CHEMBL3404056 | 118122 | None | 0 | Human | Functional | pEC50 | = | 9.2 | 9.2 | - | 1 | Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay |
ChEMBL | 438 | 7 | 1 | 2 | 6.4 | N[C@H](CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1)C1CCCCC1 | 10.1016/j.bmcl.2015.02.038 | ||
| 118727606 | 117569 | None | 0 | Human | Functional | pEC50 | = | 9.2 | 9.2 | - | 1 | Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay |
ChEMBL | 414 | 8 | 1 | 3 | 4.9 | CO[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 | 10.1016/j.bmcl.2015.02.038 | ||
| CHEMBL3400198 | 117569 | None | 0 | Human | Functional | pEC50 | = | 9.2 | 9.2 | - | 1 | Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay |
ChEMBL | 414 | 8 | 1 | 3 | 4.9 | CO[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 | 10.1016/j.bmcl.2015.02.038 | ||
| 118727605 | 117568 | None | 0 | Human | Functional | pEC50 | = | 9.0 | 9.0 | - | 1 | Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay |
ChEMBL | 398 | 7 | 1 | 2 | 5.5 | CC(C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 | 10.1016/j.bmcl.2015.02.038 | ||
| CHEMBL3400197 | 117568 | None | 0 | Human | Functional | pEC50 | = | 9.0 | 9.0 | - | 1 | Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay |
ChEMBL | 398 | 7 | 1 | 2 | 5.5 | CC(C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 | 10.1016/j.bmcl.2015.02.038 | ||
| 118730162 | 118115 | None | 0 | Human | Functional | pEC50 | = | 8.9 | 8.9 | - | 1 | Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay |
ChEMBL | 414 | 9 | 1 | 2 | 5.9 | CC(C)C[C@H](N)CN(C(=O)C(C)Cc1ccccc1)c1ccc(-c2ccccc2)cc1 | 10.1016/j.bmcl.2015.02.038 | ||
| CHEMBL3404049 | 118115 | None | 0 | Human | Functional | pEC50 | = | 8.9 | 8.9 | - | 1 | Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay |
ChEMBL | 414 | 9 | 1 | 2 | 5.9 | CC(C)C[C@H](N)CN(C(=O)C(C)Cc1ccccc1)c1ccc(-c2ccccc2)cc1 | 10.1016/j.bmcl.2015.02.038 | ||
| 118727608 | 117571 | None | 0 | Human | Functional | pEC50 | = | 8.9 | 8.9 | - | 1 | Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay |
ChEMBL | 384 | 6 | 1 | 2 | 5.2 | CC(C)(N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 | 10.1016/j.bmcl.2015.02.038 | ||
| CHEMBL3400200 | 117571 | None | 0 | Human | Functional | pEC50 | = | 8.9 | 8.9 | - | 1 | Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay |
ChEMBL | 384 | 6 | 1 | 2 | 5.2 | CC(C)(N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 | 10.1016/j.bmcl.2015.02.038 | ||
| 118730167 | 118120 | None | 0 | Human | Functional | pEC50 | = | 8.9 | 8.9 | - | 1 | Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay |
ChEMBL | 412 | 8 | 1 | 2 | 5.9 | CC[C@@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 | 10.1016/j.bmcl.2015.02.038 | ||
| CHEMBL3404054 | 118120 | None | 0 | Human | Functional | pEC50 | = | 8.9 | 8.9 | - | 1 | Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay |
ChEMBL | 412 | 8 | 1 | 2 | 5.9 | CC[C@@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 | 10.1016/j.bmcl.2015.02.038 | ||
| 118730168 | 118121 | None | 0 | Human | Functional | pEC50 | = | 8.8 | 8.8 | - | 1 | Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay |
ChEMBL | 452 | 8 | 1 | 2 | 6.8 | N[C@@H](CC1CCCCC1)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 | 10.1016/j.bmcl.2015.02.038 | ||
| CHEMBL3404055 | 118121 | None | 0 | Human | Functional | pEC50 | = | 8.8 | 8.8 | - | 1 | Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay |
ChEMBL | 452 | 8 | 1 | 2 | 6.8 | N[C@@H](CC1CCCCC1)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 | 10.1016/j.bmcl.2015.02.038 | ||
| 118730164 | 118117 | None | 0 | Human | Functional | pEC50 | = | 8.7 | 8.7 | - | 1 | Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay |
ChEMBL | 412 | 8 | 1 | 2 | 5.9 | CC(C)C[C@@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 | 10.1016/j.bmcl.2015.02.038 | ||
| CHEMBL3404051 | 118117 | None | 0 | Human | Functional | pEC50 | = | 8.7 | 8.7 | - | 1 | Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay |
ChEMBL | 412 | 8 | 1 | 2 | 5.9 | CC(C)C[C@@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccccc1)c1ccc(-c2ccccc2)cc1 | 10.1016/j.bmcl.2015.02.038 | ||
| 118727610 | 117573 | None | 0 | Human | Functional | pEC50 | = | 8 | 8.0 | - | 1 | Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay |
ChEMBL | 410 | 6 | 1 | 2 | 5.5 | O=C([C@@H]1C[C@H]1c1ccccc1)N(CC1CCCNC1)c1ccc(-c2ccccc2)cc1 | 10.1016/j.bmcl.2015.02.038 | ||
| CHEMBL3400202 | 117573 | None | 0 | Human | Functional | pEC50 | = | 8 | 8.0 | - | 1 | Agonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assayAgonist activity at GPR88 (unknown origin) transfected into cells assessed as cAMP accumulation by HTRF assay |
ChEMBL | 410 | 6 | 1 | 2 | 5.5 | O=C([C@@H]1C[C@H]1c1ccccc1)N(CC1CCCNC1)c1ccc(-c2ccccc2)cc1 | 10.1016/j.bmcl.2015.02.038 | ||
| 12395 | 3411 | None | 1 | Human | Functional | pEC50 | = | 8.0 | 8.0 | 14 | 2 | Agonist activity at PPLS-HA tagged GPR88 (unknown origin) expressed in CHO cells assessed as cAMP accumulation incubated for 30 mins by TR-FRET AssayAgonist activity at PPLS-HA tagged GPR88 (unknown origin) expressed in CHO cells assessed as cAMP accumulation incubated for 30 mins by TR-FRET Assay |
ChEMBL | 491 | 10 | 1 | 5 | 5.2 | N[C@@H]([C@@H](C)OC)CN(C(=O)[C@H]1[C@H](c2ccc(F)cn2)C1)c1ccc(c2ccc(OC(C)C)cc2)cc1 | 10.1021/acs.jmedchem.2c01983 | ||
| 167993640 | 3411 | None | 1 | Human | Functional | pEC50 | = | 8.0 | 8.0 | 14 | 2 | Agonist activity at PPLS-HA tagged GPR88 (unknown origin) expressed in CHO cells assessed as cAMP accumulation incubated for 30 mins by TR-FRET AssayAgonist activity at PPLS-HA tagged GPR88 (unknown origin) expressed in CHO cells assessed as cAMP accumulation incubated for 30 mins by TR-FRET Assay |
ChEMBL | 491 | 10 | 1 | 5 | 5.2 | N[C@@H]([C@@H](C)OC)CN(C(=O)[C@H]1[C@H](c2ccc(F)cn2)C1)c1ccc(c2ccc(OC(C)C)cc2)cc1 | 10.1021/acs.jmedchem.2c01983 | ||
| CHEMBL5498825 | 3411 | None | 1 | Human | Functional | pEC50 | = | 8.0 | 8.0 | 14 | 2 | Agonist activity at PPLS-HA tagged GPR88 (unknown origin) expressed in CHO cells assessed as cAMP accumulation incubated for 30 mins by TR-FRET AssayAgonist activity at PPLS-HA tagged GPR88 (unknown origin) expressed in CHO cells assessed as cAMP accumulation incubated for 30 mins by TR-FRET Assay |
ChEMBL | 491 | 10 | 1 | 5 | 5.2 | N[C@@H]([C@@H](C)OC)CN(C(=O)[C@H]1[C@H](c2ccc(F)cn2)C1)c1ccc(c2ccc(OC(C)C)cc2)cc1 | 10.1021/acs.jmedchem.2c01983 | ||
| 10031 | 3412 | None | 10 | Human | Functional | pEC50 | = | 7 | 7.0 | 2 | 2 | Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay |
ChEMBL | 459 | 10 | 1 | 5 | 4.4 | COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N | 10.1021/acs.jmedchem.8b00566 | ||
| 134813902 | 3412 | None | 10 | Human | Functional | pEC50 | = | 7 | 7.0 | 2 | 2 | Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay |
ChEMBL | 459 | 10 | 1 | 5 | 4.4 | COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N | 10.1021/acs.jmedchem.8b00566 | ||
| CHEMBL4595209 | 3412 | None | 10 | Human | Functional | pEC50 | = | 7 | 7.0 | 2 | 2 | Agonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assayAgonist activity at GPR88 (unknown origin) expressed in PPLS-HA-GPR88 CHO cells assessed as effect on forskolin-induced cAMP accumulation after 30 mins by Eu-cAMP tracer-based TR-FRET assay |
ChEMBL | 459 | 10 | 1 | 5 | 4.4 | COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N | 10.1021/acs.jmedchem.8b00566 | ||
| 51356430 | 118057 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay |
ChEMBL | 369 | 10 | 2 | 3 | 4.5 | CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 | nan | ||
| CHEMBL3403768 | 118057 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay |
ChEMBL | 369 | 10 | 2 | 3 | 4.5 | CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 | nan | ||
| 51356141 | 118069 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay |
ChEMBL | 438 | 11 | 1 | 4 | 4.8 | CCCC(C)COc1ccc([C@H](CN2CCOCC2)NC(=O)[C@@H](C)c2ccccc2)cc1 | nan | ||
| CHEMBL3403783 | 118069 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay |
ChEMBL | 438 | 11 | 1 | 4 | 4.8 | CCCC(C)COc1ccc([C@H](CN2CCOCC2)NC(=O)[C@@H](C)c2ccccc2)cc1 | nan | ||
| 51355601 | 133759 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay |
ChEMBL | 439 | 12 | 3 | 4 | 3.9 | CCCC(C)COc1ccc([C@H](CNC(=O)[C@@H](C)N)NC(=O)[C@@H](C)c2ccccc2)cc1 | nan | ||
| CHEMBL3714989 | 133759 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay |
ChEMBL | 439 | 12 | 3 | 4 | 3.9 | CCCC(C)COc1ccc([C@H](CNC(=O)[C@@H](C)N)NC(=O)[C@@H](C)c2ccccc2)cc1 | nan | ||
| 51355320 | 133787 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay |
ChEMBL | 438 | 14 | 2 | 3 | 6.1 | CCCC(C)COc1ccc([C@H](CNCC(C)CC)NC(=O)[C@@H](C)c2ccccc2)cc1 | nan | ||
| CHEMBL3715058 | 133787 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay |
ChEMBL | 438 | 14 | 2 | 3 | 6.1 | CCCC(C)COc1ccc([C@H](CNCC(C)CC)NC(=O)[C@@H](C)c2ccccc2)cc1 | nan | ||
| 51356142 | 133809 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay |
ChEMBL | 369 | 9 | 2 | 3 | 4.5 | CC[C@H](C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)[C@@H](C)O)cc1 | nan | ||
| CHEMBL3715126 | 133809 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay |
ChEMBL | 369 | 9 | 2 | 3 | 4.5 | CC[C@H](C)COc1ccc([C@@H](NC(=O)[C@@H](C)c2ccccc2)[C@@H](C)O)cc1 | nan | ||
| 51355319 | 133824 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay |
ChEMBL | 451 | 13 | 3 | 4 | 4.8 | CCCC(C)COc1ccc([C@H](CNC[C@@H]2CCCN2)NC(=O)[C@@H](C)c2ccccc2)cc1 | nan | ||
| CHEMBL3715177 | 133824 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay |
ChEMBL | 451 | 13 | 3 | 4 | 4.8 | CCCC(C)COc1ccc([C@H](CNC[C@@H]2CCCN2)NC(=O)[C@@H](C)c2ccccc2)cc1 | nan | ||
| 51356138 | 133851 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay |
ChEMBL | 425 | 13 | 3 | 4 | 4.4 | CCCC(C)COc1ccc([C@H](CNC[C@H](C)N)NC(=O)[C@@H](C)c2ccccc2)cc1 | nan | ||
| CHEMBL3715294 | 133851 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay |
ChEMBL | 425 | 13 | 3 | 4 | 4.4 | CCCC(C)COc1ccc([C@H](CNC[C@H](C)N)NC(=O)[C@@H](C)c2ccccc2)cc1 | nan | ||
| 58466420 | 133891 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay |
ChEMBL | 385 | 11 | 3 | 4 | 3.4 | CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](CO)c2ccccc2)cc1 | nan | ||
| CHEMBL3715473 | 133891 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay |
ChEMBL | 385 | 11 | 3 | 4 | 3.4 | CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](CO)c2ccccc2)cc1 | nan | ||
| 51356137 | 133930 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay |
ChEMBL | 459 | 13 | 2 | 4 | 5.6 | CCCC(C)COc1ccc([C@H](CNCc2cccnc2)NC(=O)[C@@H](C)c2ccccc2)cc1 | nan | ||
| CHEMBL3715603 | 133930 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay |
ChEMBL | 459 | 13 | 2 | 4 | 5.6 | CCCC(C)COc1ccc([C@H](CNCc2cccnc2)NC(=O)[C@@H](C)c2ccccc2)cc1 | nan | ||
| 51355600 | 133936 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay |
ChEMBL | 467 | 14 | 3 | 4 | 4.7 | CCCC(C)COc1ccc([C@H](CNC(=O)[C@H](N)CCC)NC(=O)[C@@H](C)c2ccccc2)cc1 | nan | ||
| CHEMBL3715622 | 133936 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay |
ChEMBL | 467 | 14 | 3 | 4 | 4.7 | CCCC(C)COc1ccc([C@H](CNC(=O)[C@H](N)CCC)NC(=O)[C@@H](C)c2ccccc2)cc1 | nan | ||
| 51356431 | 134041 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay |
ChEMBL | 448 | 13 | 3 | 4 | 5.0 | CCCC(C)COc1ccc([C@H](CNCc2cc[nH]n2)NC(=O)[C@@H](C)c2ccccc2)cc1 | nan | ||
| CHEMBL3715982 | 134041 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay |
ChEMBL | 448 | 13 | 3 | 4 | 5.0 | CCCC(C)COc1ccc([C@H](CNCc2cc[nH]n2)NC(=O)[C@@H](C)c2ccccc2)cc1 | nan | ||
| 51355324 | 134064 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay |
ChEMBL | 383 | 11 | 2 | 3 | 4.8 | CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](CC)c2ccccc2)cc1 | nan | ||
| CHEMBL3716055 | 134064 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Modulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assayModulator activity at G-protein-coupled receptor 88 (unknown origin) incubated for 1 hr by [35S]GTPgammaS binding assay |
ChEMBL | 383 | 11 | 2 | 3 | 4.8 | CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](CC)c2ccccc2)cc1 | nan | ||
Showing 1 to 50 of 1,287 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
| |
| 172463593 | 197511 | None | 0 | Human | Binding | pEC50 | = | 5 | 5.0 | - | 0 | Displacement of [35S]GTPgammaS from PPLS-HA tagged human GPR88 overexpressed in CHO cells membrane incubated for 60 mins radioligand binding assayDisplacement of [35S]GTPgammaS from PPLS-HA tagged human GPR88 overexpressed in CHO cells membrane incubated for 60 mins radioligand binding assay |
ChEMBL | 459 | 10 | 1 | 5 | 4.4 | COCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)OC)C(=O)[C@H]3C[C@@H]3c3ccccn3)cc2)cc1 | 10.1021/acs.jmedchem.2c01983 | ||
| CHEMBL5429768 | 197511 | None | 0 | Human | Binding | pEC50 | = | 5 | 5.0 | - | 0 | Displacement of [35S]GTPgammaS from PPLS-HA tagged human GPR88 overexpressed in CHO cells membrane incubated for 60 mins radioligand binding assayDisplacement of [35S]GTPgammaS from PPLS-HA tagged human GPR88 overexpressed in CHO cells membrane incubated for 60 mins radioligand binding assay |
ChEMBL | 459 | 10 | 1 | 5 | 4.4 | COCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)OC)C(=O)[C@H]3C[C@@H]3c3ccccn3)cc2)cc1 | 10.1021/acs.jmedchem.2c01983 | ||
| CHEMBL5499810 | 197511 | None | 0 | Human | Binding | pEC50 | = | 5 | 5.0 | - | 0 | Displacement of [35S]GTPgammaS from PPLS-HA tagged human GPR88 overexpressed in CHO cells membrane incubated for 60 mins radioligand binding assayDisplacement of [35S]GTPgammaS from PPLS-HA tagged human GPR88 overexpressed in CHO cells membrane incubated for 60 mins radioligand binding assay |
ChEMBL | 459 | 10 | 1 | 5 | 4.4 | COCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)OC)C(=O)[C@H]3C[C@@H]3c3ccccn3)cc2)cc1 | 10.1021/acs.jmedchem.2c01983 | ||
| 12395 | 3411 | None | 1 | Human | Binding | pEC50 | = | 7.9 | 7.9 | - | 0 | Displacement of [35S]GTPgammaS from PPLS-HA tagged human GPR88 overexpressed in CHO cells membrane incubated for 60 mins radioligand binding assayDisplacement of [35S]GTPgammaS from PPLS-HA tagged human GPR88 overexpressed in CHO cells membrane incubated for 60 mins radioligand binding assay |
ChEMBL | 491 | 10 | 1 | 5 | 5.2 | N[C@@H]([C@@H](C)OC)CN(C(=O)[C@H]1[C@H](c2ccc(F)cn2)C1)c1ccc(c2ccc(OC(C)C)cc2)cc1 | 10.1021/acs.jmedchem.2c01983 | ||
| 167993640 | 3411 | None | 1 | Human | Binding | pEC50 | = | 7.9 | 7.9 | - | 0 | Displacement of [35S]GTPgammaS from PPLS-HA tagged human GPR88 overexpressed in CHO cells membrane incubated for 60 mins radioligand binding assayDisplacement of [35S]GTPgammaS from PPLS-HA tagged human GPR88 overexpressed in CHO cells membrane incubated for 60 mins radioligand binding assay |
ChEMBL | 491 | 10 | 1 | 5 | 5.2 | N[C@@H]([C@@H](C)OC)CN(C(=O)[C@H]1[C@H](c2ccc(F)cn2)C1)c1ccc(c2ccc(OC(C)C)cc2)cc1 | 10.1021/acs.jmedchem.2c01983 | ||
| CHEMBL5498825 | 3411 | None | 1 | Human | Binding | pEC50 | = | 7.9 | 7.9 | - | 0 | Displacement of [35S]GTPgammaS from PPLS-HA tagged human GPR88 overexpressed in CHO cells membrane incubated for 60 mins radioligand binding assayDisplacement of [35S]GTPgammaS from PPLS-HA tagged human GPR88 overexpressed in CHO cells membrane incubated for 60 mins radioligand binding assay |
ChEMBL | 491 | 10 | 1 | 5 | 5.2 | N[C@@H]([C@@H](C)OC)CN(C(=O)[C@H]1[C@H](c2ccc(F)cn2)C1)c1ccc(c2ccc(OC(C)C)cc2)cc1 | 10.1021/acs.jmedchem.2c01983 | ||
| 12395 | 3411 | None | 1 | Mouse | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | Displacement of [35S]GTPgammaS from mouse striatal membrane GPR88 incubated for 60 mins by radioligand binding assayDisplacement of [35S]GTPgammaS from mouse striatal membrane GPR88 incubated for 60 mins by radioligand binding assay |
ChEMBL | 491 | 10 | 1 | 5 | 5.2 | N[C@@H]([C@@H](C)OC)CN(C(=O)[C@H]1[C@H](c2ccc(F)cn2)C1)c1ccc(c2ccc(OC(C)C)cc2)cc1 | 10.1021/acs.jmedchem.2c01983 | ||
| 167993640 | 3411 | None | 1 | Mouse | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | Displacement of [35S]GTPgammaS from mouse striatal membrane GPR88 incubated for 60 mins by radioligand binding assayDisplacement of [35S]GTPgammaS from mouse striatal membrane GPR88 incubated for 60 mins by radioligand binding assay |
ChEMBL | 491 | 10 | 1 | 5 | 5.2 | N[C@@H]([C@@H](C)OC)CN(C(=O)[C@H]1[C@H](c2ccc(F)cn2)C1)c1ccc(c2ccc(OC(C)C)cc2)cc1 | 10.1021/acs.jmedchem.2c01983 | ||
| CHEMBL5498825 | 3411 | None | 1 | Mouse | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | Displacement of [35S]GTPgammaS from mouse striatal membrane GPR88 incubated for 60 mins by radioligand binding assayDisplacement of [35S]GTPgammaS from mouse striatal membrane GPR88 incubated for 60 mins by radioligand binding assay |
ChEMBL | 491 | 10 | 1 | 5 | 5.2 | N[C@@H]([C@@H](C)OC)CN(C(=O)[C@H]1[C@H](c2ccc(F)cn2)C1)c1ccc(c2ccc(OC(C)C)cc2)cc1 | 10.1021/acs.jmedchem.2c01983 | ||
| 134128290 | 194406 | None | 3 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 1 | Agonist activity at GPR88 (unknown origin) transfected in HEK293 cells assessed as cAMP level by GloSensor cAMP assayAgonist activity at GPR88 (unknown origin) transfected in HEK293 cells assessed as cAMP level by GloSensor cAMP assay |
ChEMBL | 455 | 10 | 1 | 3 | 6.2 | CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@H]3C[C@@H]3c3ccccn3)cc2)cc1 | 10.1016/j.bmcl.2022.129120 | ||
| CHEMBL5285428 | 194406 | None | 3 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 1 | Agonist activity at GPR88 (unknown origin) transfected in HEK293 cells assessed as cAMP level by GloSensor cAMP assayAgonist activity at GPR88 (unknown origin) transfected in HEK293 cells assessed as cAMP level by GloSensor cAMP assay |
ChEMBL | 455 | 10 | 1 | 3 | 6.2 | CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@H]3C[C@@H]3c3ccccn3)cc2)cc1 | 10.1016/j.bmcl.2022.129120 | ||
| 51356430 | 118057 | None | 0 | Human | Binding | pEC50 | = | 6.7 | 6.7 | - | 1 | Agonist activity at GPR88 (unknown origin) transfected in HEK293 cells assessed as cAMP level by GloSensor cAMP assayAgonist activity at GPR88 (unknown origin) transfected in HEK293 cells assessed as cAMP level by GloSensor cAMP assay |
ChEMBL | 369 | 10 | 2 | 3 | 4.5 | CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 | 10.1016/j.bmcl.2022.129120 | ||
| CHEMBL3403768 | 118057 | None | 0 | Human | Binding | pEC50 | = | 6.7 | 6.7 | - | 1 | Agonist activity at GPR88 (unknown origin) transfected in HEK293 cells assessed as cAMP level by GloSensor cAMP assayAgonist activity at GPR88 (unknown origin) transfected in HEK293 cells assessed as cAMP level by GloSensor cAMP assay |
ChEMBL | 369 | 10 | 2 | 3 | 4.5 | CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 | 10.1016/j.bmcl.2022.129120 | ||
| 58466401 | 118066 | None | 0 | Human | Binding | pEC50 | = | 6.5 | 6.5 | - | 1 | Agonist activity at GPR88 (unknown origin) transfected in HEK293 cells assessed as cAMP level by GloSensor cAMP assayAgonist activity at GPR88 (unknown origin) transfected in HEK293 cells assessed as cAMP level by GloSensor cAMP assay |
ChEMBL | 368 | 10 | 2 | 3 | 4.4 | CCCC(C)COc1ccc([C@H](CN)NC(=O)[C@@H](C)c2ccccc2)cc1 | 10.1016/j.bmcl.2022.129120 | ||
| CHEMBL3403780 | 118066 | None | 0 | Human | Binding | pEC50 | = | 6.5 | 6.5 | - | 1 | Agonist activity at GPR88 (unknown origin) transfected in HEK293 cells assessed as cAMP level by GloSensor cAMP assayAgonist activity at GPR88 (unknown origin) transfected in HEK293 cells assessed as cAMP level by GloSensor cAMP assay |
ChEMBL | 368 | 10 | 2 | 3 | 4.4 | CCCC(C)COc1ccc([C@H](CN)NC(=O)[C@@H](C)c2ccccc2)cc1 | 10.1016/j.bmcl.2022.129120 | ||
| CHEMBL3884102 | 118066 | None | 0 | Human | Binding | pEC50 | = | 6.5 | 6.5 | - | 1 | Agonist activity at GPR88 (unknown origin) transfected in HEK293 cells assessed as cAMP level by GloSensor cAMP assayAgonist activity at GPR88 (unknown origin) transfected in HEK293 cells assessed as cAMP level by GloSensor cAMP assay |
ChEMBL | 368 | 10 | 2 | 3 | 4.4 | CCCC(C)COc1ccc([C@H](CN)NC(=O)[C@@H](C)c2ccccc2)cc1 | 10.1016/j.bmcl.2022.129120 | ||
| 10031 | 3412 | None | 10 | Human | Binding | pEC50 | = | 7.4 | 7.4 | -3 | 3 | Agonist activity at GPR88 (unknown origin) transfected in HEK293 cells assessed as cAMP level by GloSensor cAMP assayAgonist activity at GPR88 (unknown origin) transfected in HEK293 cells assessed as cAMP level by GloSensor cAMP assay |
ChEMBL | 459 | 10 | 1 | 5 | 4.4 | COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N | 10.1016/j.bmcl.2022.129120 | ||
| 134813902 | 3412 | None | 10 | Human | Binding | pEC50 | = | 7.4 | 7.4 | -3 | 3 | Agonist activity at GPR88 (unknown origin) transfected in HEK293 cells assessed as cAMP level by GloSensor cAMP assayAgonist activity at GPR88 (unknown origin) transfected in HEK293 cells assessed as cAMP level by GloSensor cAMP assay |
ChEMBL | 459 | 10 | 1 | 5 | 4.4 | COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N | 10.1016/j.bmcl.2022.129120 | ||
| CHEMBL4595209 | 3412 | None | 10 | Human | Binding | pEC50 | = | 7.4 | 7.4 | -3 | 3 | Agonist activity at GPR88 (unknown origin) transfected in HEK293 cells assessed as cAMP level by GloSensor cAMP assayAgonist activity at GPR88 (unknown origin) transfected in HEK293 cells assessed as cAMP level by GloSensor cAMP assay |
ChEMBL | 459 | 10 | 1 | 5 | 4.4 | COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N | 10.1016/j.bmcl.2022.129120 | ||
| 10031 | 3412 | None | 10 | Human | Binding | pEC50 | = | 7.2 | 7.2 | -3 | 3 | Displacement of [35S]GTPgammaS from PPLS-HA tagged human GPR88 overexpressed in CHO cells membrane incubated for 60 mins radioligand binding assayDisplacement of [35S]GTPgammaS from PPLS-HA tagged human GPR88 overexpressed in CHO cells membrane incubated for 60 mins radioligand binding assay |
ChEMBL | 459 | 10 | 1 | 5 | 4.4 | COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N | 10.1021/acs.jmedchem.2c01983 | ||
| 134813902 | 3412 | None | 10 | Human | Binding | pEC50 | = | 7.2 | 7.2 | -3 | 3 | Displacement of [35S]GTPgammaS from PPLS-HA tagged human GPR88 overexpressed in CHO cells membrane incubated for 60 mins radioligand binding assayDisplacement of [35S]GTPgammaS from PPLS-HA tagged human GPR88 overexpressed in CHO cells membrane incubated for 60 mins radioligand binding assay |
ChEMBL | 459 | 10 | 1 | 5 | 4.4 | COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N | 10.1021/acs.jmedchem.2c01983 | ||
| CHEMBL4595209 | 3412 | None | 10 | Human | Binding | pEC50 | = | 7.2 | 7.2 | -3 | 3 | Displacement of [35S]GTPgammaS from PPLS-HA tagged human GPR88 overexpressed in CHO cells membrane incubated for 60 mins radioligand binding assayDisplacement of [35S]GTPgammaS from PPLS-HA tagged human GPR88 overexpressed in CHO cells membrane incubated for 60 mins radioligand binding assay |
ChEMBL | 459 | 10 | 1 | 5 | 4.4 | COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N | 10.1021/acs.jmedchem.2c01983 | ||
| 58466521 | 1064 | None | 6 | Human | Binding | pEC50 | = | 7.1 | 7.1 | - | 1 | Agonist activity at GPR88 (unknown origin) transfected in HEK293 cells assessed as cAMP level by GloSensor cAMP assayAgonist activity at GPR88 (unknown origin) transfected in HEK293 cells assessed as cAMP level by GloSensor cAMP assay |
ChEMBL | 455 | 10 | 1 | 3 | 6.2 | CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N | 10.1016/j.bmcl.2022.129120 | ||
| 7798 | 1064 | None | 6 | Human | Binding | pEC50 | = | 7.1 | 7.1 | - | 1 | Agonist activity at GPR88 (unknown origin) transfected in HEK293 cells assessed as cAMP level by GloSensor cAMP assayAgonist activity at GPR88 (unknown origin) transfected in HEK293 cells assessed as cAMP level by GloSensor cAMP assay |
ChEMBL | 455 | 10 | 1 | 3 | 6.2 | CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N | 10.1016/j.bmcl.2022.129120 | ||
| CHEMBL3401461 | 1064 | None | 6 | Human | Binding | pEC50 | = | 7.1 | 7.1 | - | 1 | Agonist activity at GPR88 (unknown origin) transfected in HEK293 cells assessed as cAMP level by GloSensor cAMP assayAgonist activity at GPR88 (unknown origin) transfected in HEK293 cells assessed as cAMP level by GloSensor cAMP assay |
ChEMBL | 455 | 10 | 1 | 3 | 6.2 | CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N | 10.1016/j.bmcl.2022.129120 | ||
| 58466401 | 118066 | None | 0 | Mouse | Binding | pEC50 | = | 6.0 | 6.0 | - | 1 | Agonist activity at GPR88 in mouse striatal membranes assessed as increase in [35S]-GTP-gammaS bindingAgonist activity at GPR88 in mouse striatal membranes assessed as increase in [35S]-GTP-gammaS binding |
ChEMBL | 368 | 10 | 2 | 3 | 4.4 | CCCC(C)COc1ccc([C@H](CN)NC(=O)[C@@H](C)c2ccccc2)cc1 | 10.1016/j.bmc.2016.11.058 | ||
| CHEMBL3403780 | 118066 | None | 0 | Mouse | Binding | pEC50 | = | 6.0 | 6.0 | - | 1 | Agonist activity at GPR88 in mouse striatal membranes assessed as increase in [35S]-GTP-gammaS bindingAgonist activity at GPR88 in mouse striatal membranes assessed as increase in [35S]-GTP-gammaS binding |
ChEMBL | 368 | 10 | 2 | 3 | 4.4 | CCCC(C)COc1ccc([C@H](CN)NC(=O)[C@@H](C)c2ccccc2)cc1 | 10.1016/j.bmc.2016.11.058 | ||
| CHEMBL3884102 | 118066 | None | 0 | Mouse | Binding | pEC50 | = | 6.0 | 6.0 | - | 1 | Agonist activity at GPR88 in mouse striatal membranes assessed as increase in [35S]-GTP-gammaS bindingAgonist activity at GPR88 in mouse striatal membranes assessed as increase in [35S]-GTP-gammaS binding |
ChEMBL | 368 | 10 | 2 | 3 | 4.4 | CCCC(C)COc1ccc([C@H](CN)NC(=O)[C@@H](C)c2ccccc2)cc1 | 10.1016/j.bmc.2016.11.058 | ||
| 172469753 | 197560 | None | 0 | Human | Binding | pEC50 | = | 5.0 | 5.0 | - | 0 | Displacement of [35S]GTPgammaS from PPLS-HA tagged human GPR88 overexpressed in CHO cells membrane incubated for 60 mins radioligand binding assayDisplacement of [35S]GTPgammaS from PPLS-HA tagged human GPR88 overexpressed in CHO cells membrane incubated for 60 mins radioligand binding assay |
ChEMBL | 491 | 10 | 1 | 5 | 5.2 | CO[C@H](C)[C@H](N)CN(C(=O)[C@H]1C[C@@H]1c1ccc(F)cn1)c1ccc(-c2ccc(OC(C)C)cc2)cc1 | 10.1021/acs.jmedchem.2c01983 | ||
| CHEMBL5437290 | 197560 | None | 0 | Human | Binding | pEC50 | = | 5.0 | 5.0 | - | 0 | Displacement of [35S]GTPgammaS from PPLS-HA tagged human GPR88 overexpressed in CHO cells membrane incubated for 60 mins radioligand binding assayDisplacement of [35S]GTPgammaS from PPLS-HA tagged human GPR88 overexpressed in CHO cells membrane incubated for 60 mins radioligand binding assay |
ChEMBL | 491 | 10 | 1 | 5 | 5.2 | CO[C@H](C)[C@H](N)CN(C(=O)[C@H]1C[C@@H]1c1ccc(F)cn1)c1ccc(-c2ccc(OC(C)C)cc2)cc1 | 10.1021/acs.jmedchem.2c01983 | ||
| CHEMBL5500144 | 197560 | None | 0 | Human | Binding | pEC50 | = | 5.0 | 5.0 | - | 0 | Displacement of [35S]GTPgammaS from PPLS-HA tagged human GPR88 overexpressed in CHO cells membrane incubated for 60 mins radioligand binding assayDisplacement of [35S]GTPgammaS from PPLS-HA tagged human GPR88 overexpressed in CHO cells membrane incubated for 60 mins radioligand binding assay |
ChEMBL | 491 | 10 | 1 | 5 | 5.2 | CO[C@H](C)[C@H](N)CN(C(=O)[C@H]1C[C@@H]1c1ccc(F)cn1)c1ccc(-c2ccc(OC(C)C)cc2)cc1 | 10.1021/acs.jmedchem.2c01983 | ||
| 10031 | 3412 | None | 10 | Mouse | Binding | pKd | = | 7.4 | 7.4 | 3 | 3 | Binding affinity to GPR88 in mouse striatal membrane by filtration methodBinding affinity to GPR88 in mouse striatal membrane by filtration method |
ChEMBL | 459 | 10 | 1 | 5 | 4.4 | COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N | 10.1016/j.bmcl.2022.129120 | ||
| 134813902 | 3412 | None | 10 | Mouse | Binding | pKd | = | 7.4 | 7.4 | 3 | 3 | Binding affinity to GPR88 in mouse striatal membrane by filtration methodBinding affinity to GPR88 in mouse striatal membrane by filtration method |
ChEMBL | 459 | 10 | 1 | 5 | 4.4 | COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N | 10.1016/j.bmcl.2022.129120 | ||
| CHEMBL4595209 | 3412 | None | 10 | Mouse | Binding | pKd | = | 7.4 | 7.4 | 3 | 3 | Binding affinity to GPR88 in mouse striatal membrane by filtration methodBinding affinity to GPR88 in mouse striatal membrane by filtration method |
ChEMBL | 459 | 10 | 1 | 5 | 4.4 | COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N | 10.1016/j.bmcl.2022.129120 | ||
| 10031 | 3412 | None | 10 | Human | Binding | pKd | = | 7.1 | 7.1 | -3 | 3 | Binding affinity to PPLS-HA tagged human GPR88 expressed in CHO cell membrane by filtration methodBinding affinity to PPLS-HA tagged human GPR88 expressed in CHO cell membrane by filtration method |
ChEMBL | 459 | 10 | 1 | 5 | 4.4 | COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N | 10.1016/j.bmcl.2022.129120 | ||
| 134813902 | 3412 | None | 10 | Human | Binding | pKd | = | 7.1 | 7.1 | -3 | 3 | Binding affinity to PPLS-HA tagged human GPR88 expressed in CHO cell membrane by filtration methodBinding affinity to PPLS-HA tagged human GPR88 expressed in CHO cell membrane by filtration method |
ChEMBL | 459 | 10 | 1 | 5 | 4.4 | COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N | 10.1016/j.bmcl.2022.129120 | ||
| CHEMBL4595209 | 3412 | None | 10 | Human | Binding | pKd | = | 7.1 | 7.1 | -3 | 3 | Binding affinity to PPLS-HA tagged human GPR88 expressed in CHO cell membrane by filtration methodBinding affinity to PPLS-HA tagged human GPR88 expressed in CHO cell membrane by filtration method |
ChEMBL | 459 | 10 | 1 | 5 | 4.4 | COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N | 10.1016/j.bmcl.2022.129120 | ||
| 58466401 | 118066 | None | 0 | Human | Binding | pKi | = | 6.7 | 6.7 | - | 1 | Displacement of [3H]RTI-33 from GPR88 (unknown origin) by competition binding assayDisplacement of [3H]RTI-33 from GPR88 (unknown origin) by competition binding assay |
ChEMBL | 368 | 10 | 2 | 3 | 4.4 | CCCC(C)COc1ccc([C@H](CN)NC(=O)[C@@H](C)c2ccccc2)cc1 | 10.1016/j.bmcl.2022.129120 | ||
| CHEMBL3403780 | 118066 | None | 0 | Human | Binding | pKi | = | 6.7 | 6.7 | - | 1 | Displacement of [3H]RTI-33 from GPR88 (unknown origin) by competition binding assayDisplacement of [3H]RTI-33 from GPR88 (unknown origin) by competition binding assay |
ChEMBL | 368 | 10 | 2 | 3 | 4.4 | CCCC(C)COc1ccc([C@H](CN)NC(=O)[C@@H](C)c2ccccc2)cc1 | 10.1016/j.bmcl.2022.129120 | ||
| CHEMBL3884102 | 118066 | None | 0 | Human | Binding | pKi | = | 6.7 | 6.7 | - | 1 | Displacement of [3H]RTI-33 from GPR88 (unknown origin) by competition binding assayDisplacement of [3H]RTI-33 from GPR88 (unknown origin) by competition binding assay |
ChEMBL | 368 | 10 | 2 | 3 | 4.4 | CCCC(C)COc1ccc([C@H](CN)NC(=O)[C@@H](C)c2ccccc2)cc1 | 10.1016/j.bmcl.2022.129120 | ||
| 10031 | 3412 | None | 10 | Human | Binding | pKi | = | 6.7 | 6.7 | -3 | 3 | Displacement of [3H]RTI-33 from GPR88 (unknown origin) by competition binding assayDisplacement of [3H]RTI-33 from GPR88 (unknown origin) by competition binding assay |
ChEMBL | 459 | 10 | 1 | 5 | 4.4 | COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N | 10.1016/j.bmcl.2022.129120 | ||
| 134813902 | 3412 | None | 10 | Human | Binding | pKi | = | 6.7 | 6.7 | -3 | 3 | Displacement of [3H]RTI-33 from GPR88 (unknown origin) by competition binding assayDisplacement of [3H]RTI-33 from GPR88 (unknown origin) by competition binding assay |
ChEMBL | 459 | 10 | 1 | 5 | 4.4 | COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N | 10.1016/j.bmcl.2022.129120 | ||
| CHEMBL4595209 | 3412 | None | 10 | Human | Binding | pKi | = | 6.7 | 6.7 | -3 | 3 | Displacement of [3H]RTI-33 from GPR88 (unknown origin) by competition binding assayDisplacement of [3H]RTI-33 from GPR88 (unknown origin) by competition binding assay |
ChEMBL | 459 | 10 | 1 | 5 | 4.4 | COCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](OC)C)N | 10.1016/j.bmcl.2022.129120 | ||
| 58466521 | 1064 | None | 6 | Human | Binding | pKi | = | 6.6 | 6.6 | - | 1 | Displacement of [3H]RTI-33 from GPR88 (unknown origin) by competition binding assayDisplacement of [3H]RTI-33 from GPR88 (unknown origin) by competition binding assay |
ChEMBL | 455 | 10 | 1 | 3 | 6.2 | CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N | 10.1016/j.bmcl.2022.129120 | ||
| 7798 | 1064 | None | 6 | Human | Binding | pKi | = | 6.6 | 6.6 | - | 1 | Displacement of [3H]RTI-33 from GPR88 (unknown origin) by competition binding assayDisplacement of [3H]RTI-33 from GPR88 (unknown origin) by competition binding assay |
ChEMBL | 455 | 10 | 1 | 3 | 6.2 | CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N | 10.1016/j.bmcl.2022.129120 | ||
| CHEMBL3401461 | 1064 | None | 6 | Human | Binding | pKi | = | 6.6 | 6.6 | - | 1 | Displacement of [3H]RTI-33 from GPR88 (unknown origin) by competition binding assayDisplacement of [3H]RTI-33 from GPR88 (unknown origin) by competition binding assay |
ChEMBL | 455 | 10 | 1 | 3 | 6.2 | CCCc1ccc(cc1)c1ccc(cc1)N(C(=O)[C@@H]1C[C@H]1c1ccccn1)C[C@H]([C@H](CC)C)N | 10.1016/j.bmcl.2022.129120 | ||
| 134128290 | 194406 | None | 3 | Human | Binding | pKi | = | 6.3 | 6.3 | - | 1 | Displacement of [3H]RTI-33 from GPR88 (unknown origin) by competition binding assayDisplacement of [3H]RTI-33 from GPR88 (unknown origin) by competition binding assay |
ChEMBL | 455 | 10 | 1 | 3 | 6.2 | CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@H]3C[C@@H]3c3ccccn3)cc2)cc1 | 10.1016/j.bmcl.2022.129120 | ||
| CHEMBL5285428 | 194406 | None | 3 | Human | Binding | pKi | = | 6.3 | 6.3 | - | 1 | Displacement of [3H]RTI-33 from GPR88 (unknown origin) by competition binding assayDisplacement of [3H]RTI-33 from GPR88 (unknown origin) by competition binding assay |
ChEMBL | 455 | 10 | 1 | 3 | 6.2 | CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@H]3C[C@@H]3c3ccccn3)cc2)cc1 | 10.1016/j.bmcl.2022.129120 | ||
| 51356430 | 118057 | None | 0 | Human | Binding | pKi | = | 6.2 | 6.2 | - | 1 | Displacement of [3H]RTI-33 from GPR88 (unknown origin) by competition binding assayDisplacement of [3H]RTI-33 from GPR88 (unknown origin) by competition binding assay |
ChEMBL | 369 | 10 | 2 | 3 | 4.5 | CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 | 10.1016/j.bmcl.2022.129120 | ||
| CHEMBL3403768 | 118057 | None | 0 | Human | Binding | pKi | = | 6.2 | 6.2 | - | 1 | Displacement of [3H]RTI-33 from GPR88 (unknown origin) by competition binding assayDisplacement of [3H]RTI-33 from GPR88 (unknown origin) by competition binding assay |
ChEMBL | 369 | 10 | 2 | 3 | 4.5 | CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1 | 10.1016/j.bmcl.2022.129120 | ||
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