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
| |
| 156013464 | 177602 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production |
ChEMBL | 486 | 6 | 2 | 7 | 4.7 | CCOc1cc(Cl)c(C(=O)NC(=O)Nc2ncc(-c3ccccc3)s2)cc1N1CCOCC1 | 10.1016/j.bmcl.2020.126953 | ||
| CHEMBL4639430 | 177602 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production |
ChEMBL | 486 | 6 | 2 | 7 | 4.7 | CCOc1cc(Cl)c(C(=O)NC(=O)Nc2ncc(-c3ccccc3)s2)cc1N1CCOCC1 | 10.1016/j.bmcl.2020.126953 | ||
| 58345681 | 134516 | None | 1 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay |
ChEMBL | 226 | 1 | 2 | 5 | 1.7 | Nc1nc2ccc(O)nc2n1-c1ccccc1 | nan | ||
| CHEMBL3717589 | 134516 | None | 1 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assayAgonist activity at human GPR81 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by HTRF assay |
ChEMBL | 226 | 1 | 2 | 5 | 1.7 | Nc1nc2ccc(O)nc2n1-c1ccccc1 | nan | ||
| 156019324 | 178079 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | 14 | 2 | Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production |
ChEMBL | 530 | 7 | 1 | 8 | 4.9 | CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(OC4CCN(C)CC4)cc3s2)cc1N1CCOCC1 | 10.1016/j.bmcl.2020.126953 | ||
| CHEMBL4646005 | 178079 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | 14 | 2 | Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production |
ChEMBL | 530 | 7 | 1 | 8 | 4.9 | CCOc1cc(Cl)c(C(=O)Nc2nc3ccc(OC4CCN(C)CC4)cc3s2)cc1N1CCOCC1 | 10.1016/j.bmcl.2020.126953 | ||
| 145985690 | 165538 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | 1 | 3 | Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production |
ChEMBL | 464 | 5 | 2 | 7 | 3.9 | CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3c(s2)CCCC3)cc1N1CCOCC1 | 10.1016/j.bmcl.2020.126953 | ||
| CHEMBL4239086 | 165538 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | 1 | 3 | Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production |
ChEMBL | 464 | 5 | 2 | 7 | 3.9 | CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3c(s2)CCCC3)cc1N1CCOCC1 | 10.1016/j.bmcl.2020.126953 | ||
| 156009938 | 177142 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production |
ChEMBL | 556 | 7 | 2 | 8 | 4.7 | CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(CN4CCN(C)CC4)cc3s2)cc1N1CCCC1 | 10.1016/j.bmcl.2020.126953 | ||
| CHEMBL4632482 | 177142 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human GPR81 overexpressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production |
ChEMBL | 556 | 7 | 2 | 8 | 4.7 | CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3ccc(CN4CCN(C)CC4)cc3s2)cc1N1CCCC1 | 10.1016/j.bmcl.2020.126953 | ||
| 58345670 | 134829 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 313 | 1 | 1 | 4 | 3.8 | Oc1ccc2ncn(-c3ccc(Cl)cc3C(F)(F)F)c2n1 | nan | ||
| CHEMBL3718634 | 134829 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 313 | 1 | 1 | 4 | 3.8 | Oc1ccc2ncn(-c3ccc(Cl)cc3C(F)(F)F)c2n1 | nan | ||
| 58345743 | 133712 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 328 | 1 | 2 | 5 | 3.7 | Nc1nc2ccc(O)nc2n1-c1ccc(Cl)c(Cl)c1Cl | nan | ||
| CHEMBL3714817 | 133712 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 328 | 1 | 2 | 5 | 3.7 | Nc1nc2ccc(O)nc2n1-c1ccc(Cl)c(Cl)c1Cl | nan | ||
| 58345768 | 133726 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 285 | 2 | 1 | 4 | 3.7 | Oc1ccc2nc(C3CC3)n(-c3ccccc3Cl)c2n1 | nan | ||
| CHEMBL3714879 | 133726 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 285 | 2 | 1 | 4 | 3.7 | Oc1ccc2nc(C3CC3)n(-c3ccccc3Cl)c2n1 | nan | ||
| 58345668 | 133727 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 304 | 1 | 2 | 5 | 2.5 | Nc1nc2ccc(O)nc2n1-c1ccc(Br)cc1 | nan | ||
| CHEMBL3714885 | 133727 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 304 | 1 | 2 | 5 | 2.5 | Nc1nc2ccc(O)nc2n1-c1ccc(Br)cc1 | nan | ||
| 58345728 | 133734 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 347 | 1 | 1 | 4 | 4.2 | Oc1ccc2ncn(-c3ccc(C(F)(F)F)cc3C(F)(F)F)c2n1 | nan | ||
| CHEMBL3714909 | 133734 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 347 | 1 | 1 | 4 | 4.2 | Oc1ccc2ncn(-c3ccc(C(F)(F)F)cc3C(F)(F)F)c2n1 | nan | ||
| 58345725 | 133750 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 367 | 1 | 1 | 4 | 3.7 | Oc1ccc2nc(Br)n(-c3ccccc3Br)c2n1 | nan | ||
| CHEMBL3714960 | 133750 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 367 | 1 | 1 | 4 | 3.7 | Oc1ccc2nc(Br)n(-c3ccccc3Br)c2n1 | nan | ||
| 58345654 | 133753 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 243 | 1 | 1 | 4 | 2.6 | Cc1cc(F)ccc1-n1cnc2ccc(O)nc21 | nan | ||
| CHEMBL3714970 | 133753 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 243 | 1 | 1 | 4 | 2.6 | Cc1cc(F)ccc1-n1cnc2ccc(O)nc21 | nan | ||
| 58345758 | 133767 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 278 | 1 | 2 | 5 | 2.5 | Nc1nc2ccc(O)nc2n1-c1cccc(F)c1Cl | nan | ||
| CHEMBL3715004 | 133767 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 278 | 1 | 2 | 5 | 2.5 | Nc1nc2ccc(O)nc2n1-c1cccc(F)c1Cl | nan | ||
| 58345741 | 133773 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 239 | 1 | 1 | 4 | 2.7 | Cc1ccc(-n2c(C)nc3ccc(O)nc32)cc1 | nan | ||
| CHEMBL3715017 | 133773 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 239 | 1 | 1 | 4 | 2.7 | Cc1ccc(-n2c(C)nc3ccc(O)nc32)cc1 | nan | ||
| 58345706 | 133792 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 253 | 3 | 1 | 4 | 3.1 | CCCc1nc2ccc(O)nc2n1-c1ccccc1 | nan | ||
| CHEMBL3715077 | 133792 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 253 | 3 | 1 | 4 | 3.1 | CCCc1nc2ccc(O)nc2n1-c1ccccc1 | nan | ||
| 58345750 | 133815 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 255 | 1 | 1 | 6 | 1.9 | Oc1ccc2ncn(-c3ccc4c(c3)OCO4)c2n1 | nan | ||
| CHEMBL3715155 | 133815 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 255 | 1 | 1 | 6 | 1.9 | Oc1ccc2ncn(-c3ccc4c(c3)OCO4)c2n1 | nan | ||
| 58345653 | 133823 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 303 | 1 | 1 | 4 | 3.2 | Cc1nc2ccc(O)nc2n1-c1ccccc1Br | nan | ||
| CHEMBL3715174 | 133823 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 303 | 1 | 1 | 4 | 3.2 | Cc1nc2ccc(O)nc2n1-c1ccccc1Br | nan | ||
| 58345739 | 133835 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 247 | 1 | 1 | 4 | 2.4 | Oc1ccc2ncn(-c3cccc(F)c3F)c2n1 | nan | ||
| CHEMBL3715218 | 133835 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 247 | 1 | 1 | 4 | 2.4 | Oc1ccc2ncn(-c3cccc(F)c3F)c2n1 | nan | ||
| 58345704 | 133862 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 245 | 1 | 1 | 4 | 3.4 | Oc1ccc2ncn(C3CCCCCCC3)c2n1 | nan | ||
| CHEMBL3715359 | 133862 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 245 | 1 | 1 | 4 | 3.4 | Oc1ccc2ncn(C3CCCCCCC3)c2n1 | nan | ||
| 58345713 | 133863 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 328 | 1 | 2 | 5 | 3.7 | Nc1nc2ccc(O)nc2n1-c1cc(Cl)c(Cl)cc1Cl | nan | ||
| CHEMBL3715361 | 133863 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 328 | 1 | 2 | 5 | 3.7 | Nc1nc2ccc(O)nc2n1-c1cc(Cl)c(Cl)cc1Cl | nan | ||
| 58345751 | 133871 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 244 | 1 | 2 | 5 | 1.8 | Nc1nc2ccc(O)nc2n1-c1ccccc1F | nan | ||
| CHEMBL3715394 | 133871 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 244 | 1 | 2 | 5 | 1.8 | Nc1nc2ccc(O)nc2n1-c1ccccc1F | nan | ||
| 58345683 | 133892 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 295 | 2 | 1 | 5 | 3.0 | Oc1ccc2ncn(-c3ccccc3OC(F)(F)F)c2n1 | nan | ||
| CHEMBL3715478 | 133892 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 295 | 2 | 1 | 5 | 3.0 | Oc1ccc2ncn(-c3ccccc3OC(F)(F)F)c2n1 | nan | ||
| 58345724 | 133907 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 253 | 1 | 1 | 4 | 3.1 | Cc1cccc(-n2c(C)nc3ccc(O)nc32)c1C | nan | ||
| CHEMBL3715536 | 133907 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 253 | 1 | 1 | 4 | 3.1 | Cc1cccc(-n2c(C)nc3ccc(O)nc32)c1C | nan | ||
| 58345682 | 133915 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 275 | 1 | 1 | 4 | 3.6 | Cc1nc2ccc(O)nc2n1-c1cccc2ccccc12 | nan | ||
| CHEMBL3715558 | 133915 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 275 | 1 | 1 | 4 | 3.6 | Cc1nc2ccc(O)nc2n1-c1cccc2ccccc12 | nan | ||
| 58345677 | 133919 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 284 | 1 | 2 | 5 | 2.6 | Nc1nc2ccc(O)nc2n1C12CC3CC(CC(C3)C1)C2 | nan | ||
| CHEMBL3715572 | 133919 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Agonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assayAgonist activity at human GPR81 expressed in CHO-K1 cell membranes pre-incubated for 5 to 10 mins before [35S]GTPgammaS addition followed by further incubation for 60 mins by microbeta counting based [35S]GTPgammaS binding assay |
ChEMBL | 284 | 1 | 2 | 5 | 2.6 | Nc1nc2ccc(O)nc2n1C12CC3CC(CC(C3)C1)C2 | nan | ||
Showing 1 to 50 of 698 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
| |
| 145984458 | 165590 | None | 0 | Rat | Binding | pEC50 | = | 6 | 6.0 | - | 0 | Agonist activity at rat GPR81 expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assayAgonist activity at rat GPR81 expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assay |
ChEMBL | 600 | 7 | 2 | 8 | 4.6 | CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3c(s2)C[Si](C)(c2ccc(OC)cc2)CC3)cc1N1CCOCC1 | 10.1021/acs.jmedchem.7b00718 | ||
| CHEMBL4240407 | 165590 | None | 0 | Rat | Binding | pEC50 | = | 6 | 6.0 | - | 0 | Agonist activity at rat GPR81 expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assayAgonist activity at rat GPR81 expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assay |
ChEMBL | 600 | 7 | 2 | 8 | 4.6 | CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3c(s2)C[Si](C)(c2ccc(OC)cc2)CC3)cc1N1CCOCC1 | 10.1021/acs.jmedchem.7b00718 | ||
| 145984088 | 165910 | None | 0 | Rat | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | Agonist activity at rat GPR81 expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assayAgonist activity at rat GPR81 expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assay |
ChEMBL | 630 | 8 | 2 | 9 | 4.6 | CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3c(s2)C[Si](C)(c2c(OC)cccc2OC)CC3)cc1N1CCOCC1 | 10.1021/acs.jmedchem.7b00718 | ||
| CHEMBL4248415 | 165910 | None | 0 | Rat | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | Agonist activity at rat GPR81 expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assayAgonist activity at rat GPR81 expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assay |
ChEMBL | 630 | 8 | 2 | 9 | 4.6 | CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3c(s2)C[Si](C)(c2c(OC)cccc2OC)CC3)cc1N1CCOCC1 | 10.1021/acs.jmedchem.7b00718 | ||
| 145985690 | 165538 | None | 0 | Rat | Binding | pEC50 | = | 6.6 | 6.6 | - | 0 | Agonist activity at rat GPR81 expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assayAgonist activity at rat GPR81 expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assay |
ChEMBL | 464 | 5 | 2 | 7 | 3.9 | CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3c(s2)CCCC3)cc1N1CCOCC1 | 10.1021/acs.jmedchem.7b00718 | ||
| CHEMBL4239086 | 165538 | None | 0 | Rat | Binding | pEC50 | = | 6.6 | 6.6 | - | 0 | Agonist activity at rat GPR81 expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assayAgonist activity at rat GPR81 expressed in T-REx-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin stimulation and measured after 20 mins by TR-FRET assay |
ChEMBL | 464 | 5 | 2 | 7 | 3.9 | CCOc1cc(Cl)c(C(=O)NC(=O)Nc2nc3c(s2)CCCC3)cc1N1CCOCC1 | 10.1021/acs.jmedchem.7b00718 | ||
Showing 1 to 6 of 6 entries