Ligand source activities (1 row/activity)
Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
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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
| |
13103 | 2975 | None | 0 | Human | Functional | pEC50 | = | 10.7 | 10.7 | - | 1 | Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay |
ChEMBL | 331 | 4 | 1 | 2 | 3.9 | ClC1=C(C=C(C=C1)CCCC=2C=[N+](C=C(C2)O)[O-])C(F)(F)F | 10.1021/acs.jmedchem.3c00951 | ||
171037436 | 2975 | None | 0 | Human | Functional | pEC50 | = | 10.7 | 10.7 | - | 1 | Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay |
ChEMBL | 331 | 4 | 1 | 2 | 3.9 | ClC1=C(C=C(C=C1)CCCC=2C=[N+](C=C(C2)O)[O-])C(F)(F)F | 10.1021/acs.jmedchem.3c00951 | ||
CHEMBL5395893 | 2975 | None | 0 | Human | Functional | pEC50 | = | 10.7 | 10.7 | - | 1 | Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay |
ChEMBL | 331 | 4 | 1 | 2 | 3.9 | ClC1=C(C=C(C=C1)CCCC=2C=[N+](C=C(C2)O)[O-])C(F)(F)F | 10.1021/acs.jmedchem.3c00951 | ||
13103 | 2975 | None | 0 | Human | Functional | pEC50 | = | 10.7 | 10.7 | - | 1 | Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay |
ChEMBL | 331 | 4 | 1 | 2 | 3.9 | ClC1=C(C=C(C=C1)CCCC=2C=[N+](C=C(C2)O)[O-])C(F)(F)F | 10.1021/acs.jmedchem.3c00951 | ||
171037436 | 2975 | None | 0 | Human | Functional | pEC50 | = | 10.7 | 10.7 | - | 1 | Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay |
ChEMBL | 331 | 4 | 1 | 2 | 3.9 | ClC1=C(C=C(C=C1)CCCC=2C=[N+](C=C(C2)O)[O-])C(F)(F)F | 10.1021/acs.jmedchem.3c00951 | ||
CHEMBL5395893 | 2975 | None | 0 | Human | Functional | pEC50 | = | 10.7 | 10.7 | - | 1 | Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay |
ChEMBL | 331 | 4 | 1 | 2 | 3.9 | ClC1=C(C=C(C=C1)CCCC=2C=[N+](C=C(C2)O)[O-])C(F)(F)F | 10.1021/acs.jmedchem.3c00951 | ||
11212 | 165 | None | 0 | Human | Functional | pEC50 | = | 9.7 | 9.7 | - | 1 | Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay |
ChEMBL | 237 | 8 | 2 | 2 | 3.4 | CCCCCCCCCc1cc(O)cc(=O)[nH]1 | 10.1021/acsmedchemlett.6b00025 | ||
127045422 | 165 | None | 0 | Human | Functional | pEC50 | = | 9.7 | 9.7 | - | 1 | Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay |
ChEMBL | 237 | 8 | 2 | 2 | 3.4 | CCCCCCCCCc1cc(O)cc(=O)[nH]1 | 10.1021/acsmedchemlett.6b00025 | ||
CHEMBL3828298 | 165 | None | 0 | Human | Functional | pEC50 | = | 9.7 | 9.7 | - | 1 | Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay |
ChEMBL | 237 | 8 | 2 | 2 | 3.4 | CCCCCCCCCc1cc(O)cc(=O)[nH]1 | 10.1021/acsmedchemlett.6b00025 | ||
11212 | 165 | None | 0 | Human | Functional | pEC50 | = | 9.5 | 9.5 | - | 1 | Agonist activity at GPR84 (unknown origin) expressed in in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin addition measured after 30 mins by HTRF assayAgonist activity at GPR84 (unknown origin) expressed in in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin addition measured after 30 mins by HTRF assay |
ChEMBL | 237 | 8 | 2 | 2 | 3.4 | CCCCCCCCCc1cc(O)cc(=O)[nH]1 | 10.1021/acsmedchemlett.6b00025 | ||
127045422 | 165 | None | 0 | Human | Functional | pEC50 | = | 9.5 | 9.5 | - | 1 | Agonist activity at GPR84 (unknown origin) expressed in in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin addition measured after 30 mins by HTRF assayAgonist activity at GPR84 (unknown origin) expressed in in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin addition measured after 30 mins by HTRF assay |
ChEMBL | 237 | 8 | 2 | 2 | 3.4 | CCCCCCCCCc1cc(O)cc(=O)[nH]1 | 10.1021/acsmedchemlett.6b00025 | ||
CHEMBL3828298 | 165 | None | 0 | Human | Functional | pEC50 | = | 9.5 | 9.5 | - | 1 | Agonist activity at GPR84 (unknown origin) expressed in in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin addition measured after 30 mins by HTRF assayAgonist activity at GPR84 (unknown origin) expressed in in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed by forskolin addition measured after 30 mins by HTRF assay |
ChEMBL | 237 | 8 | 2 | 2 | 3.4 | CCCCCCCCCc1cc(O)cc(=O)[nH]1 | 10.1021/acsmedchemlett.6b00025 | ||
11211 | 4154 | None | 30 | Human | Functional | pEC50 | = | 9.1 | 9.1 | -2 | 2 | Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric methodAgonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric method |
ChEMBL | 228 | 6 | 2 | 4 | 2.1 | CCCCCCSc1nc(O)cc(=O)[nH]1 | 10.1021/acs.jmedchem.9b01339 | ||
1912564 | 4154 | None | 30 | Human | Functional | pEC50 | = | 9.1 | 9.1 | -2 | 2 | Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric methodAgonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric method |
ChEMBL | 228 | 6 | 2 | 4 | 2.1 | CCCCCCSc1nc(O)cc(=O)[nH]1 | 10.1021/acs.jmedchem.9b01339 | ||
CHEMBL3827756 | 4154 | None | 30 | Human | Functional | pEC50 | = | 9.1 | 9.1 | -2 | 2 | Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric methodAgonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric method |
ChEMBL | 228 | 6 | 2 | 4 | 2.1 | CCCCCCSc1nc(O)cc(=O)[nH]1 | 10.1021/acs.jmedchem.9b01339 | ||
11211 | 4154 | None | 30 | Human | Functional | pEC50 | = | 9 | 9.0 | -2 | 2 | Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as inhibition of forskolin-induced cAMP production measured after 30 mins by HTRF assayAgonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as inhibition of forskolin-induced cAMP production measured after 30 mins by HTRF assay |
ChEMBL | 228 | 6 | 2 | 4 | 2.1 | CCCCCCSc1nc(O)cc(=O)[nH]1 | 10.1021/acs.jmedchem.9b01339 | ||
1912564 | 4154 | None | 30 | Human | Functional | pEC50 | = | 9 | 9.0 | -2 | 2 | Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as inhibition of forskolin-induced cAMP production measured after 30 mins by HTRF assayAgonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as inhibition of forskolin-induced cAMP production measured after 30 mins by HTRF assay |
ChEMBL | 228 | 6 | 2 | 4 | 2.1 | CCCCCCSc1nc(O)cc(=O)[nH]1 | 10.1021/acs.jmedchem.9b01339 | ||
CHEMBL3827756 | 4154 | None | 30 | Human | Functional | pEC50 | = | 9 | 9.0 | -2 | 2 | Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as inhibition of forskolin-induced cAMP production measured after 30 mins by HTRF assayAgonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as inhibition of forskolin-induced cAMP production measured after 30 mins by HTRF assay |
ChEMBL | 228 | 6 | 2 | 4 | 2.1 | CCCCCCSc1nc(O)cc(=O)[nH]1 | 10.1021/acs.jmedchem.9b01339 | ||
54678947 | 23048 | None | 0 | Human | Functional | pEC50 | = | 8.9 | 8.9 | - | 1 | Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay |
ChEMBL | 209 | 6 | 2 | 3 | 3.0 | CCCCCCCc1cc(O)cc(O)n1 | 10.1021/acsmedchemlett.6b00025 | ||
CHEMBL13302 | 23048 | None | 0 | Human | Functional | pEC50 | = | 8.9 | 8.9 | - | 1 | Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay |
ChEMBL | 209 | 6 | 2 | 3 | 3.0 | CCCCCCCc1cc(O)cc(O)n1 | 10.1021/acsmedchemlett.6b00025 | ||
127044155 | 141237 | None | 0 | Human | Functional | pEC50 | = | 8.9 | 8.9 | - | 1 | Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay |
ChEMBL | 223 | 7 | 2 | 3 | 3.4 | CCCCCCCCc1cc(O)cc(O)n1 | 10.1021/acsmedchemlett.6b00025 | ||
CHEMBL3827638 | 141237 | None | 0 | Human | Functional | pEC50 | = | 8.9 | 8.9 | - | 1 | Agonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assayAgonist activity at GPR84 (unknown origin) expressed in HEK293 cells coexpressing Galpha16 protein by Fluo-4 AM dye based calcium mobilization assay |
ChEMBL | 223 | 7 | 2 | 3 | 3.4 | CCCCCCCCc1cc(O)cc(O)n1 | 10.1021/acsmedchemlett.6b00025 | ||
23646340 | 84356 | None | 0 | Human | Functional | pEC50 | = | 8.8 | 8.8 | - | 1 | Agonist activity at hemagglutinin-tagged human GPR84 expressed in HEK293 cells assessed as inhibition of forskolin induced cAMP production incubated for 60 mins by HTRF assayAgonist activity at hemagglutinin-tagged human GPR84 expressed in HEK293 cells assessed as inhibition of forskolin induced cAMP production incubated for 60 mins by HTRF assay |
ChEMBL | 252 | 7 | 2 | 4 | 3.1 | CCCCCCCCC1=C(O)C(=O)C=C(O)C1=O | 10.1021/acs.jmedchem.3c00951 | ||
CHEMBL221598 | 84356 | None | 0 | Human | Functional | pEC50 | = | 8.8 | 8.8 | - | 1 | Agonist activity at hemagglutinin-tagged human GPR84 expressed in HEK293 cells assessed as inhibition of forskolin induced cAMP production incubated for 60 mins by HTRF assayAgonist activity at hemagglutinin-tagged human GPR84 expressed in HEK293 cells assessed as inhibition of forskolin induced cAMP production incubated for 60 mins by HTRF assay |
ChEMBL | 252 | 7 | 2 | 4 | 3.1 | CCCCCCCCC1=C(O)C(=O)C=C(O)C1=O | 10.1021/acs.jmedchem.3c00951 | ||
23646340 | 84356 | None | 0 | Human | Functional | pEC50 | = | 8.8 | 8.8 | - | 1 | Agonist activity at human GPR84 expressed in HEK293 cells assessed as reduction in forskolin-stimulated cAMP production incubated for 60 mins by HTRF assayAgonist activity at human GPR84 expressed in HEK293 cells assessed as reduction in forskolin-stimulated cAMP production incubated for 60 mins by HTRF assay |
ChEMBL | 252 | 7 | 2 | 4 | 3.1 | CCCCCCCCC1=C(O)C(=O)C=C(O)C1=O | 10.1021/acs.jmedchem.0c01378 | ||
CHEMBL221598 | 84356 | None | 0 | Human | Functional | pEC50 | = | 8.8 | 8.8 | - | 1 | Agonist activity at human GPR84 expressed in HEK293 cells assessed as reduction in forskolin-stimulated cAMP production incubated for 60 mins by HTRF assayAgonist activity at human GPR84 expressed in HEK293 cells assessed as reduction in forskolin-stimulated cAMP production incubated for 60 mins by HTRF assay |
ChEMBL | 252 | 7 | 2 | 4 | 3.1 | CCCCCCCCC1=C(O)C(=O)C=C(O)C1=O | 10.1021/acs.jmedchem.0c01378 | ||
172463022 | 196536 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay |
ChEMBL | 289 | 5 | 0 | 2 | 3.5 | [O-][n+]1cccc(CCOc2ccc(Cl)c(C3CC3)c2)c1 | 10.1021/acs.jmedchem.3c00951 | ||
CHEMBL5426206 | 196536 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as inhibition of forskolin induced cAMP production pretreated with forskolin for 30 mins followed by compound addition and measured after 18 to 24 hrs by DiscoverX HitHunter cAMP assay |
ChEMBL | 289 | 5 | 0 | 2 | 3.5 | [O-][n+]1cccc(CCOc2ccc(Cl)c(C3CC3)c2)c1 | 10.1021/acs.jmedchem.3c00951 | ||
133081959 | 3213 | None | 2 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Agonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as beta-arrestin recruitment treated for 90 mins by luminescence based assayAgonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as beta-arrestin recruitment treated for 90 mins by luminescence based assay |
ChEMBL | 309 | 4 | 3 | 3 | 1.5 | Brc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 | 10.1021/acs.jmedchem.3c00951 | ||
9871 | 3213 | None | 2 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Agonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as beta-arrestin recruitment treated for 90 mins by luminescence based assayAgonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as beta-arrestin recruitment treated for 90 mins by luminescence based assay |
ChEMBL | 309 | 4 | 3 | 3 | 1.5 | Brc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 | 10.1021/acs.jmedchem.3c00951 | ||
CHEMBL4444010 | 3213 | None | 2 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Agonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as beta-arrestin recruitment treated for 90 mins by luminescence based assayAgonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as beta-arrestin recruitment treated for 90 mins by luminescence based assay |
ChEMBL | 309 | 4 | 3 | 3 | 1.5 | Brc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 | 10.1021/acs.jmedchem.3c00951 | ||
11208 | 1423 | None | 70 | Human | Functional | pEC50 | = | 6 | 6.0 | 2 | 2 | Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric methodAgonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric method |
ChEMBL | 246 | 2 | 2 | 0 | 4.2 | c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 | 10.1021/acs.jmedchem.9b01339 | ||
3071 | 1423 | None | 70 | Human | Functional | pEC50 | = | 6 | 6.0 | 2 | 2 | Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric methodAgonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric method |
ChEMBL | 246 | 2 | 2 | 0 | 4.2 | c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 | 10.1021/acs.jmedchem.9b01339 | ||
CHEMBL446452 | 1423 | None | 70 | Human | Functional | pEC50 | = | 6 | 6.0 | 2 | 2 | Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric methodAgonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric method |
ChEMBL | 246 | 2 | 2 | 0 | 4.2 | c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 | 10.1021/acs.jmedchem.9b01339 | ||
DB11875 | 1423 | None | 70 | Human | Functional | pEC50 | = | 6 | 6.0 | 2 | 2 | Agonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric methodAgonist activity at recombinant human N-terminal epitope tagged/C-terminal eYFP-fused FLAG-tagged GPR84 expressed in Flp-In TREx 293 cell membranes assessed as stimulation of [35S]GTPgammaS binding preincubated for 15 mins followed by [35S]GTPgammaS addition and measured 45 mins by liquid scintillation spectrometric method |
ChEMBL | 246 | 2 | 2 | 0 | 4.2 | c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 | 10.1021/acs.jmedchem.9b01339 | ||
137656606 | 159702 | None | 0 | Human | Functional | pEC50 | = | 5 | 5.0 | - | 1 | Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay |
ChEMBL | 304 | 3 | 2 | 2 | 4.0 | COC(=O)c1ccc2[nH]cc(Cc3c[nH]c4ccccc34)c2c1 | 10.1021/acs.jmedchem.6b01593 | ||
CHEMBL4103279 | 159702 | None | 0 | Human | Functional | pEC50 | = | 5 | 5.0 | - | 1 | Agonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assayAgonist activity at Gi coupled human GPR84 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 15 mins in presence of [3H]-cAMP by radiometric assay |
ChEMBL | 304 | 3 | 2 | 2 | 4.0 | COC(=O)c1ccc2[nH]cc(Cc3c[nH]c4ccccc34)c2c1 | 10.1021/acs.jmedchem.6b01593 | ||
3893 | 2287 | None | 65 | Human | Functional | pEC50 | = | 5.0 | 5.0 | -3 | 4 | Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting methodAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting method |
ChEMBL | 200 | 10 | 1 | 1 | 4.0 | CCCCCCCCCCCC(=O)O | 10.1039/C7MD00130D | ||
4642 | 2287 | None | 65 | Human | Functional | pEC50 | = | 5.0 | 5.0 | -3 | 4 | Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting methodAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting method |
ChEMBL | 200 | 10 | 1 | 1 | 4.0 | CCCCCCCCCCCC(=O)O | 10.1039/C7MD00130D | ||
5534 | 2287 | None | 65 | Human | Functional | pEC50 | = | 5.0 | 5.0 | -3 | 4 | Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting methodAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting method |
ChEMBL | 200 | 10 | 1 | 1 | 4.0 | CCCCCCCCCCCC(=O)O | 10.1039/C7MD00130D | ||
CHEMBL108766 | 2287 | None | 65 | Human | Functional | pEC50 | = | 5.0 | 5.0 | -3 | 4 | Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting methodAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting method |
ChEMBL | 200 | 10 | 1 | 1 | 4.0 | CCCCCCCCCCCC(=O)O | 10.1039/C7MD00130D | ||
DB03017 | 2287 | None | 65 | Human | Functional | pEC50 | = | 5.0 | 5.0 | -3 | 4 | Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting methodAgonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting method |
ChEMBL | 200 | 10 | 1 | 1 | 4.0 | CCCCCCCCCCCC(=O)O | 10.1039/C7MD00130D | ||
10354234 | 164 | None | 39 | Human | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | Agonist activity at recombinant human GPR84 expressed in HEK293 cells co-expressing Gqi5 assessed as increase in myo-[3H]inositol phosphate accumulation measured after 2 hrs by topcount scintillation counting methodAgonist activity at recombinant human GPR84 expressed in HEK293 cells co-expressing Gqi5 assessed as increase in myo-[3H]inositol phosphate accumulation measured after 2 hrs by topcount scintillation counting method |
ChEMBL | 239 | 8 | 3 | 3 | 1.8 | CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 | 10.1021/acs.jmedchem.9b01339 | ||
5846 | 164 | None | 39 | Human | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | Agonist activity at recombinant human GPR84 expressed in HEK293 cells co-expressing Gqi5 assessed as increase in myo-[3H]inositol phosphate accumulation measured after 2 hrs by topcount scintillation counting methodAgonist activity at recombinant human GPR84 expressed in HEK293 cells co-expressing Gqi5 assessed as increase in myo-[3H]inositol phosphate accumulation measured after 2 hrs by topcount scintillation counting method |
ChEMBL | 239 | 8 | 3 | 3 | 1.8 | CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 | 10.1021/acs.jmedchem.9b01339 | ||
CHEMBL3827832 | 164 | None | 39 | Human | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | Agonist activity at recombinant human GPR84 expressed in HEK293 cells co-expressing Gqi5 assessed as increase in myo-[3H]inositol phosphate accumulation measured after 2 hrs by topcount scintillation counting methodAgonist activity at recombinant human GPR84 expressed in HEK293 cells co-expressing Gqi5 assessed as increase in myo-[3H]inositol phosphate accumulation measured after 2 hrs by topcount scintillation counting method |
ChEMBL | 239 | 8 | 3 | 3 | 1.8 | CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 | 10.1021/acs.jmedchem.9b01339 | ||
3893 | 2287 | None | 65 | Human | Functional | pEC50 | = | 5.0 | 5.0 | -3 | 4 | Agonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting methodAgonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting method |
ChEMBL | 200 | 10 | 1 | 1 | 4.0 | CCCCCCCCCCCC(=O)O | 10.1021/acs.jmedchem.0c01378 | ||
4642 | 2287 | None | 65 | Human | Functional | pEC50 | = | 5.0 | 5.0 | -3 | 4 | Agonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting methodAgonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting method |
ChEMBL | 200 | 10 | 1 | 1 | 4.0 | CCCCCCCCCCCC(=O)O | 10.1021/acs.jmedchem.0c01378 | ||
5534 | 2287 | None | 65 | Human | Functional | pEC50 | = | 5.0 | 5.0 | -3 | 4 | Agonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting methodAgonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting method |
ChEMBL | 200 | 10 | 1 | 1 | 4.0 | CCCCCCCCCCCC(=O)O | 10.1021/acs.jmedchem.0c01378 | ||
CHEMBL108766 | 2287 | None | 65 | Human | Functional | pEC50 | = | 5.0 | 5.0 | -3 | 4 | Agonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting methodAgonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting method |
ChEMBL | 200 | 10 | 1 | 1 | 4.0 | CCCCCCCCCCCC(=O)O | 10.1021/acs.jmedchem.0c01378 | ||
DB03017 | 2287 | None | 65 | Human | Functional | pEC50 | = | 5.0 | 5.0 | -3 | 4 | Agonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting methodAgonist activity at human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS incorporation incubated for 1 hr by liquid scintillation counting method |
ChEMBL | 200 | 10 | 1 | 1 | 4.0 | CCCCCCCCCCCC(=O)O | 10.1021/acs.jmedchem.0c01378 |
Showing 1 to 50 of 2,113 entries
Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
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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
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Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
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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
| |
135373094 | 1357 | None | 64 | Human | Binding | pEC50 | = | 5 | 5.0 | - | 1 | Agonist activity at human GPR84 assessed as beta-arrestin recruitment by beta-galactosidase complementation assayAgonist activity at human GPR84 assessed as beta-arrestin recruitment by beta-galactosidase complementation assay |
ChEMBL | 172 | 8 | 1 | 1 | 3.2 | CCCCCCCCCC(=O)O | 10.1021/acs.jmedchem.6b01593 | ||
2969 | 1357 | None | 64 | Human | Binding | pEC50 | = | 5 | 5.0 | - | 1 | Agonist activity at human GPR84 assessed as beta-arrestin recruitment by beta-galactosidase complementation assayAgonist activity at human GPR84 assessed as beta-arrestin recruitment by beta-galactosidase complementation assay |
ChEMBL | 172 | 8 | 1 | 1 | 3.2 | CCCCCCCCCC(=O)O | 10.1021/acs.jmedchem.6b01593 | ||
5532 | 1357 | None | 64 | Human | Binding | pEC50 | = | 5 | 5.0 | - | 1 | Agonist activity at human GPR84 assessed as beta-arrestin recruitment by beta-galactosidase complementation assayAgonist activity at human GPR84 assessed as beta-arrestin recruitment by beta-galactosidase complementation assay |
ChEMBL | 172 | 8 | 1 | 1 | 3.2 | CCCCCCCCCC(=O)O | 10.1021/acs.jmedchem.6b01593 | ||
CHEMBL107498 | 1357 | None | 64 | Human | Binding | pEC50 | = | 5 | 5.0 | - | 1 | Agonist activity at human GPR84 assessed as beta-arrestin recruitment by beta-galactosidase complementation assayAgonist activity at human GPR84 assessed as beta-arrestin recruitment by beta-galactosidase complementation assay |
ChEMBL | 172 | 8 | 1 | 1 | 3.2 | CCCCCCCCCC(=O)O | 10.1021/acs.jmedchem.6b01593 | ||
DB03600 | 1357 | None | 64 | Human | Binding | pEC50 | = | 5 | 5.0 | - | 1 | Agonist activity at human GPR84 assessed as beta-arrestin recruitment by beta-galactosidase complementation assayAgonist activity at human GPR84 assessed as beta-arrestin recruitment by beta-galactosidase complementation assay |
ChEMBL | 172 | 8 | 1 | 1 | 3.2 | CCCCCCCCCC(=O)O | 10.1021/acs.jmedchem.6b01593 | ||
135373094 | 1357 | None | 64 | Human | Binding | pEC50 | = | 5 | 5.0 | - | 1 | Agonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment by beta-galactosidase based PathHunter assay |
ChEMBL | 172 | 8 | 1 | 1 | 3.2 | CCCCCCCCCC(=O)O | 10.1021/acs.jmedchem.9b01339 | ||
2969 | 1357 | None | 64 | Human | Binding | pEC50 | = | 5 | 5.0 | - | 1 | Agonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment by beta-galactosidase based PathHunter assay |
ChEMBL | 172 | 8 | 1 | 1 | 3.2 | CCCCCCCCCC(=O)O | 10.1021/acs.jmedchem.9b01339 | ||
5532 | 1357 | None | 64 | Human | Binding | pEC50 | = | 5 | 5.0 | - | 1 | Agonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment by beta-galactosidase based PathHunter assay |
ChEMBL | 172 | 8 | 1 | 1 | 3.2 | CCCCCCCCCC(=O)O | 10.1021/acs.jmedchem.9b01339 | ||
CHEMBL107498 | 1357 | None | 64 | Human | Binding | pEC50 | = | 5 | 5.0 | - | 1 | Agonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment by beta-galactosidase based PathHunter assay |
ChEMBL | 172 | 8 | 1 | 1 | 3.2 | CCCCCCCCCC(=O)O | 10.1021/acs.jmedchem.9b01339 | ||
DB03600 | 1357 | None | 64 | Human | Binding | pEC50 | = | 5 | 5.0 | - | 1 | Agonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment by beta-galactosidase based PathHunter assay |
ChEMBL | 172 | 8 | 1 | 1 | 3.2 | CCCCCCCCCC(=O)O | 10.1021/acs.jmedchem.9b01339 | ||
9944370 | 93566 | None | 3 | Human | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method |
ChEMBL | 306 | 4 | 2 | 2 | 4.3 | COc1ccc2[nH]cc(Cc3c[nH]c4ccc(OC)cc34)c2c1 | 10.1021/acs.jmedchem.9b01339 | ||
CHEMBL246298 | 93566 | None | 3 | Human | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method |
ChEMBL | 306 | 4 | 2 | 2 | 4.3 | COc1ccc2[nH]cc(Cc3c[nH]c4ccc(OC)cc34)c2c1 | 10.1021/acs.jmedchem.9b01339 | ||
137649817 | 157503 | None | 0 | Human | Binding | pEC50 | = | 5.0 | 5.0 | - | 0 | Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay |
ChEMBL | 318 | 2 | 2 | 0 | 4.8 | Fc1cc2[nH]cc(Cc3c[nH]c4cc(F)c(F)cc34)c2cc1F | 10.1021/acs.jmedchem.6b01593 | ||
CHEMBL4078546 | 157503 | None | 0 | Human | Binding | pEC50 | = | 5.0 | 5.0 | - | 0 | Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay |
ChEMBL | 318 | 2 | 2 | 0 | 4.8 | Fc1cc2[nH]cc(Cc3c[nH]c4cc(F)c(F)cc34)c2cc1F | 10.1021/acs.jmedchem.6b01593 | ||
133081959 | 3213 | None | 2 | Human | Binding | pEC50 | = | 7.0 | 7.0 | - | 1 | Agonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay |
ChEMBL | 309 | 4 | 3 | 3 | 1.5 | Brc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 | 10.1021/acs.jmedchem.9b01339 | ||
9871 | 3213 | None | 2 | Human | Binding | pEC50 | = | 7.0 | 7.0 | - | 1 | Agonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay |
ChEMBL | 309 | 4 | 3 | 3 | 1.5 | Brc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 | 10.1021/acs.jmedchem.9b01339 | ||
CHEMBL4444010 | 3213 | None | 2 | Human | Binding | pEC50 | = | 7.0 | 7.0 | - | 1 | Agonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay |
ChEMBL | 309 | 4 | 3 | 3 | 1.5 | Brc1ccc(cc1)CCNc1cc(=O)[nH]c(=O)[nH]1 | 10.1021/acs.jmedchem.9b01339 | ||
137649231 | 157227 | None | 0 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay |
ChEMBL | 264 | 2 | 2 | 0 | 4.4 | Fc1ccc2[nH]cc(Cc3c[nH]c4ccccc34)c2c1 | 10.1021/acs.jmedchem.6b01593 | ||
CHEMBL4075099 | 157227 | None | 0 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay |
ChEMBL | 264 | 2 | 2 | 0 | 4.4 | Fc1ccc2[nH]cc(Cc3c[nH]c4ccccc34)c2c1 | 10.1021/acs.jmedchem.6b01593 | ||
10354234 | 164 | None | 39 | Human | Binding | pEC50 | = | 5.0 | 5.0 | - | 1 | Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as induction of beta-arrestin recruitment by luminescence assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as induction of beta-arrestin recruitment by luminescence assay |
ChEMBL | 239 | 8 | 3 | 3 | 1.8 | CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 | 10.1021/acs.jmedchem.0c01378 | ||
5846 | 164 | None | 39 | Human | Binding | pEC50 | = | 5.0 | 5.0 | - | 1 | Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as induction of beta-arrestin recruitment by luminescence assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as induction of beta-arrestin recruitment by luminescence assay |
ChEMBL | 239 | 8 | 3 | 3 | 1.8 | CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 | 10.1021/acs.jmedchem.0c01378 | ||
CHEMBL3827832 | 164 | None | 39 | Human | Binding | pEC50 | = | 5.0 | 5.0 | - | 1 | Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as induction of beta-arrestin recruitment by luminescence assayAgonist activity at human GPR84 expressed in CHO-K1 cells assessed as induction of beta-arrestin recruitment by luminescence assay |
ChEMBL | 239 | 8 | 3 | 3 | 1.8 | CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 | 10.1021/acs.jmedchem.0c01378 | ||
10354234 | 164 | None | 39 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 1 | Agonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay |
ChEMBL | 239 | 8 | 3 | 3 | 1.8 | CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 | 10.1021/acs.jmedchem.9b01339 | ||
5846 | 164 | None | 39 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 1 | Agonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay |
ChEMBL | 239 | 8 | 3 | 3 | 1.8 | CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 | 10.1021/acs.jmedchem.9b01339 | ||
CHEMBL3827832 | 164 | None | 39 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 1 | Agonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay |
ChEMBL | 239 | 8 | 3 | 3 | 1.8 | CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 | 10.1021/acs.jmedchem.9b01339 | ||
9944370 | 93566 | None | 3 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay |
ChEMBL | 306 | 4 | 2 | 2 | 4.3 | COc1ccc2[nH]cc(Cc3c[nH]c4ccc(OC)cc34)c2c1 | 10.1021/acs.jmedchem.6b01593 | ||
CHEMBL246298 | 93566 | None | 3 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay |
ChEMBL | 306 | 4 | 2 | 2 | 4.3 | COc1ccc2[nH]cc(Cc3c[nH]c4ccc(OC)cc34)c2c1 | 10.1021/acs.jmedchem.6b01593 | ||
137658671 | 159542 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay |
ChEMBL | 282 | 2 | 2 | 0 | 4.5 | Fc1cccc2[nH]cc(Cc3c[nH]c4cccc(F)c34)c12 | 10.1021/acs.jmedchem.6b01593 | ||
CHEMBL4101219 | 159542 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay |
ChEMBL | 282 | 2 | 2 | 0 | 4.5 | Fc1cccc2[nH]cc(Cc3c[nH]c4cccc(F)c34)c12 | 10.1021/acs.jmedchem.6b01593 | ||
11209 | 1551 | None | 66 | Human | Binding | pEC50 | = | 4.9 | 4.9 | - | 1 | Agonist activity at human GPR84 assessed as beta-arrestin recruitment by beta-galactosidase complementation assayAgonist activity at human GPR84 assessed as beta-arrestin recruitment by beta-galactosidase complementation assay |
ChEMBL | 294 | 10 | 2 | 4 | 4.3 | CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O | 10.1021/acs.jmedchem.6b01593 | ||
3218 | 1551 | None | 66 | Human | Binding | pEC50 | = | 4.9 | 4.9 | - | 1 | Agonist activity at human GPR84 assessed as beta-arrestin recruitment by beta-galactosidase complementation assayAgonist activity at human GPR84 assessed as beta-arrestin recruitment by beta-galactosidase complementation assay |
ChEMBL | 294 | 10 | 2 | 4 | 4.3 | CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O | 10.1021/acs.jmedchem.6b01593 | ||
CHEMBL221137 | 1551 | None | 66 | Human | Binding | pEC50 | = | 4.9 | 4.9 | - | 1 | Agonist activity at human GPR84 assessed as beta-arrestin recruitment by beta-galactosidase complementation assayAgonist activity at human GPR84 assessed as beta-arrestin recruitment by beta-galactosidase complementation assay |
ChEMBL | 294 | 10 | 2 | 4 | 4.3 | CCCCCCCCCCCC1=C(O)C(=O)C=C(C1=O)O | 10.1021/acs.jmedchem.6b01593 | ||
137658184 | 159845 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method |
ChEMBL | 350 | 2 | 2 | 0 | 5.8 | Fc1cc2c(Cc3c[nH]c4cc(Cl)c(F)cc34)c[nH]c2cc1Cl | 10.1021/acs.jmedchem.9b01339 | ||
CHEMBL4104992 | 159845 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method |
ChEMBL | 350 | 2 | 2 | 0 | 5.8 | Fc1cc2c(Cc3c[nH]c4cc(Cl)c(F)cc34)c[nH]c2cc1Cl | 10.1021/acs.jmedchem.9b01339 | ||
137658671 | 159542 | None | 0 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method |
ChEMBL | 282 | 2 | 2 | 0 | 4.5 | Fc1cccc2[nH]cc(Cc3c[nH]c4cccc(F)c34)c12 | 10.1021/acs.jmedchem.9b01339 | ||
CHEMBL4101219 | 159542 | None | 0 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method |
ChEMBL | 282 | 2 | 2 | 0 | 4.5 | Fc1cccc2[nH]cc(Cc3c[nH]c4cccc(F)c34)c12 | 10.1021/acs.jmedchem.9b01339 | ||
11208 | 1423 | None | 70 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay |
ChEMBL | 246 | 2 | 2 | 0 | 4.2 | c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 | 10.1021/acs.jmedchem.6b01593 | ||
3071 | 1423 | None | 70 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay |
ChEMBL | 246 | 2 | 2 | 0 | 4.2 | c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 | 10.1021/acs.jmedchem.6b01593 | ||
CHEMBL446452 | 1423 | None | 70 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay |
ChEMBL | 246 | 2 | 2 | 0 | 4.2 | c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 | 10.1021/acs.jmedchem.6b01593 | ||
DB11875 | 1423 | None | 70 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay |
ChEMBL | 246 | 2 | 2 | 0 | 4.2 | c1ccc2c(c1)c(c[nH]2)Cc1c[nH]c2c1cccc2 | 10.1021/acs.jmedchem.6b01593 | ||
12530 | 5793 | None | 58 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 1 | Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay |
ChEMBL | 214 | 11 | 1 | 1 | 4.4 | CCCCCCCCCCCCC(=O)O | 10.1021/acs.jmedchem.9b01339 | ||
CHEMBL107874 | 5793 | None | 58 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 1 | Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assayAgonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay |
ChEMBL | 214 | 11 | 1 | 1 | 4.4 | CCCCCCCCCCCCC(=O)O | 10.1021/acs.jmedchem.9b01339 | ||
137632827 | 156484 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method |
ChEMBL | 314 | 2 | 2 | 0 | 5.5 | Clc1cccc2[nH]cc(Cc3c[nH]c4cccc(Cl)c34)c12 | 10.1021/acs.jmedchem.9b01339 | ||
CHEMBL4066454 | 156484 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method |
ChEMBL | 314 | 2 | 2 | 0 | 5.5 | Clc1cccc2[nH]cc(Cc3c[nH]c4cccc(Cl)c34)c12 | 10.1021/acs.jmedchem.9b01339 | ||
10354234 | 164 | None | 39 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 1 | Agonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment measured after 20 mins by luciferase reporter gene assayAgonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment measured after 20 mins by luciferase reporter gene assay |
ChEMBL | 239 | 8 | 3 | 3 | 1.8 | CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 | 10.1021/acs.jmedchem.9b01339 | ||
5846 | 164 | None | 39 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 1 | Agonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment measured after 20 mins by luciferase reporter gene assayAgonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment measured after 20 mins by luciferase reporter gene assay |
ChEMBL | 239 | 8 | 3 | 3 | 1.8 | CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 | 10.1021/acs.jmedchem.9b01339 | ||
CHEMBL3827832 | 164 | None | 39 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 1 | Agonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment measured after 20 mins by luciferase reporter gene assayAgonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment measured after 20 mins by luciferase reporter gene assay |
ChEMBL | 239 | 8 | 3 | 3 | 1.8 | CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1 | 10.1021/acs.jmedchem.9b01339 | ||
12380289 | 158284 | None | 2 | Human | Binding | pEC50 | = | 4.7 | 4.7 | - | 0 | Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay |
ChEMBL | 260 | 2 | 2 | 1 | 3.9 | O=C(c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 | 10.1021/acs.jmedchem.6b01593 | ||
CHEMBL4087824 | 158284 | None | 2 | Human | Binding | pEC50 | = | 4.7 | 4.7 | - | 0 | Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assayAgonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay |
ChEMBL | 260 | 2 | 2 | 1 | 3.9 | O=C(c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 | 10.1021/acs.jmedchem.6b01593 | ||
12380289 | 158284 | None | 2 | Human | Binding | pEC50 | = | 5.7 | 5.7 | - | 0 | Positive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting methodPositive allosteric modulation of recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as increase in [3H]PSB-1584 binding measured after 6 hrs by scintillation counting method |
ChEMBL | 260 | 2 | 2 | 1 | 3.9 | O=C(c1c[nH]c2ccccc12)c1c[nH]c2ccccc12 | 10.1021/acs.jmedchem.9b01339 |
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