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Ligand source activities (1 row/activity)
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
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 | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
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 | |
[His5,D-Tyr6]GnRH | 1931 | None | 0 | Human | Binding | pKi | None | - | 8.10 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/17095587 | |
abarelix | 219 | None | 37 | Human | Binding | pKi | = | - | 9.30 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/17095587 | |
abarelix | 219 | None | 37 | Human | Binding | pKi | = | 9.49 | 8.02 | - | 1 | None | Drug Central | - | - | - | - | - | - | - | |
alarelin | 326 | None | 0 | Human | Binding | pKi | = | - | 9.18 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/26398856 | |
alarelin | 326 | None | 0 | Human | Binding | pKd | = | - | 9.55 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/26398856 | |
antarelix | 427 | None | 0 | Human | Binding | pKi | None | - | 9.60 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9300077 | |
BAY-786 | 216484 | None | 6 | Human | Binding | IC50 | = | 2400.00 | 5.62 | - | 2 | Affinity On-target Cellular interaction (Mechanistic biochemical IP1 assay (CHO cells stably expressing human GnRH-R, synthetic agonist Buserelin at EC80)) EUB0000335a GNRHR | ChEMBL | - | - | - | - | - | O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)[C@@H](C1CC1)N2S(=O)(=O)c1ccc(F)cc1 | https://dx.doi.org/10.6019/CHEMBL5210121 | |
BAY1214784 | 577 | None | 15 | Human | Binding | IC50 | = | 27.00 | 7.57 | 346 | 2 | Affinity Biochemical interaction (Tag Lite binding assay (human GnRH-R binding)) EUB0000347a GNRHR | ChEMBL | 671.1 | 6 | 1 | 6 | 5.26 | O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)[C@H](C1CC1)N2S(=O)(=O)c1ccc(F)cc1 | https://dx.doi.org/10.6019/CHEMBL5210307 | |
BAY1214784 | 577 | None | 15 | Human | Binding | IC50 | = | 21.00 | 7.68 | 346 | 2 | Affinity On-target Cellular interaction (Mechanistic biochemical IP1 assay (CHO cells stably expressing human GnRH-R, synthetic agonist Buserelin at EC80)) EUB0000347a GNRHR | ChEMBL | 671.1 | 6 | 1 | 6 | 5.26 | O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)[C@H](C1CC1)N2S(=O)(=O)c1ccc(F)cc1 | https://dx.doi.org/10.6019/CHEMBL5210121 | |
BAY1214784 | 577 | None | 15 | Human | Binding | IC50 | = | 27.00 | 7.57 | 346 | 2 | Binding assay (Tag Lite) | ChEMBL | 671.1 | 6 | 1 | 6 | 5.26 | O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)[C@H](C1CC1)N2S(=O)(=O)c1ccc(F)cc1 | https://dx.doi.org/10.6019/CHEMBL4507266 | |
BAY1214784 | 577 | None | 15 | Human | Binding | Kd | = | 5.52 | 8.26 | 346 | 2 | Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay | ChEMBL | 671.1 | 6 | 1 | 6 | 5.26 | O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)[C@H](C1CC1)N2S(=O)(=O)c1ccc(F)cc1 | https://dx.doi.org/10.1021/acs.jmedchem.0c01076 | |
BAY1214784 | 577 | None | 15 | Human | Binding | Kd | = | 9.83 | 8.01 | 346 | 2 | Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay | ChEMBL | 671.1 | 6 | 1 | 6 | 5.26 | O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)[C@H](C1CC1)N2S(=O)(=O)c1ccc(F)cc1 | https://dx.doi.org/10.1021/acs.jmedchem.0c01076 | |
BAY1214784 | 577 | None | 15 | Human | Binding | IC50 | = | 27.00 | 7.57 | 346 | 2 | Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells by TR-FRET assay | ChEMBL | 671.1 | 6 | 1 | 6 | 5.26 | O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)[C@H](C1CC1)N2S(=O)(=O)c1ccc(F)cc1 | https://dx.doi.org/10.1021/acs.jmedchem.0c01076 | |
BAY1214784 | 577 | None | 15 | Human | Binding | IC50 | = | 21.00 | 7.68 | 346 | 2 | Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay | ChEMBL | 671.1 | 6 | 1 | 6 | 5.26 | O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)[C@H](C1CC1)N2S(=O)(=O)c1ccc(F)cc1 | https://dx.doi.org/10.1021/acs.jmedchem.0c01076 | |
buserelin | 744 | None | 0 | Human | Binding | pKi | = | - | 9.70 | 57 | 3 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/26398856 | |
buserelin | 744 | None | 0 | Human | Binding | pKd | = | - | 9.96 | 57 | 3 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/26398856 | |
buserelin | 744 | None | 0 | Human | Binding | pKd | = | - | 9.96 | 57 | 3 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/26774084 | |
cetrorelix | 882 | None | 32 | Human | Binding | pKi | = | - | 9.65 | - | 3 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/17095587 | |
cetrorelix | 882 | None | 32 | Human | Binding | pKi | = | - | 9.65 | - | 3 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9300077 | |
cetrorelix | 882 | None | 32 | Human | Binding | pKi | = | - | 9.65 | - | 3 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/7649152 |
Showing 1 to 20 of 2,211 entries
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
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 | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
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 | |
5-(N,N-hexamethylene)-amiloride | 147 | None | 37 | Human | Functional | pIC50 | None | - | 4.30 | -9 | 20 | Unclassified | Guide to Pharmacology | 311.1 | 2 | 3 | 5 | 0.51 | NC(N)=NC(=O)c1nc(Cl)c(N2CCCCCC2)nc1N | https://pubmed.ncbi.nlm.nih.gov/18344315 | |
[Ac-D-2Nal1,D4CPA2,D-3Pal3,6,Leu8, D-Ala10]GnRH-II | 248 | None | 0 | Human | Functional | pIC50 | = | - | 9.18 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/19638591 | |
[D-Lys6]GnRH-II | 1446 | None | 0 | Human | Functional | pIC50 | = | - | 7.59 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/19638591 | |
[des-Gly10,D-Ala6]GnRH N-ethylamide | 1386 | None | 0 | Mouse | Functional | pIC50 | None | - | 9.90 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/1328228 | |
[Gln8]GnRH | 1808 | None | 0 | Human | Functional | pIC50 | None | - | 7.10 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/17452338 | |
[Ser8]GnRH | 3589 | None | 0 | Human | Functional | pIC50 | None | - | 6.20 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/17452338 | |
[Trp8]GnRH | 3874 | None | 0 | Human | Functional | pIC50 | None | - | 7.00 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/17452338 | |
[Tyr8]GnRH | 3898 | None | 0 | Human | Functional | pIC50 | None | - | 6.70 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/17452338 | |
abarelix | 219 | None | 37 | Human | Functional | Kd | = | 0.79 | 9.10 | - | 1 | Competitive antagonism of GnRH-induced response in the reporter gene assay | ChEMBL | - | - | - | - | - | - | https://dx.doi.org/10.1021/jm0003900 | |
abarelix | 219 | None | 37 | Human | Functional | IC50 | = | 3.50 | 8.46 | - | 1 | Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells | ChEMBL | - | - | - | - | - | - | https://dx.doi.org/10.1021/jm0003900 | |
ACYLINE | 213005 | None | 8 | Human | Functional | Kd | = | 2.51 | 8.60 | - | 1 | Competitive antagonism of GnRH-induced response in the reporter gene assay | ChEMBL | - | - | - | - | - | CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 | https://dx.doi.org/10.1021/jm0003900 | |
ACYLINE | 213005 | None | 8 | Human | Functional | IC50 | = | 6.80 | 8.17 | - | 1 | Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells | ChEMBL | - | - | - | - | - | CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 | https://dx.doi.org/10.1021/jm0003900 | |
ACYLINE | 213005 | None | 8 | Human | Functional | IC50 | = | 0.69 | 9.16 | - | 1 | Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay | ChEMBL | - | - | - | - | - | CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 | https://dx.doi.org/10.1021/jm060240a | |
ACYLINE | 213005 | None | 8 | Human | Functional | IC50 | = | 0.69 | 9.16 | - | 1 | Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay | ChEMBL | - | - | - | - | - | CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 | https://dx.doi.org/10.1021/jm060240a | |
ACYLINE | 213005 | None | 8 | Human | Functional | IC50 | = | 0.52 | 9.28 | - | 1 | Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay | ChEMBL | - | - | - | - | - | CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 | https://dx.doi.org/10.1021/jm0613931 | |
BAY-786 | 216484 | None | 6 | Human | Functional | IC50 | = | 2400.00 | 5.62 | - | 2 | Mechanistic assay measuring cellular IP1 | ChEMBL | - | - | - | - | - | O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)[C@@H](C1CC1)N2S(=O)(=O)c1ccc(F)cc1 | https://dx.doi.org/10.6019/CHEMBL4507266 | |
BAY1214784 | 577 | None | 15 | Human | Functional | pIC50 | = | - | 7.68 | 151 | 2 | Antagonism of buserelin-induced GnRHR activation in a proprietary IP-One HTRF assay | Guide to Pharmacology | 671.1 | 6 | 1 | 6 | 5.26 | O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)[C@H](C1CC1)N2S(=O)(=O)c1ccc(F)cc1 | https://pubmed.ncbi.nlm.nih.gov/32960053 | |
BAY1214784 | 577 | None | 15 | Human | Functional | IC50 | = | 21.00 | 7.68 | 151 | 2 | Mechanistic assay measuring cellular IP1 | ChEMBL | 671.1 | 6 | 1 | 6 | 5.26 | O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)[C@H](C1CC1)N2S(=O)(=O)c1ccc(F)cc1 | https://dx.doi.org/10.6019/CHEMBL4507266 | |
buserelin | 744 | None | 0 | Human | Functional | pEC50 | = | 10.52 | 7.98 | 2 | 3 | None | Drug Central | - | - | - | - | - | - | - | |
buserelin | 744 | None | 0 | Human | Functional | pEC50 | = | - | 10.52 | 2 | 3 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/26774084 |
Showing 1 to 20 of 668 entries