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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 | |
[D-Tyr8]CYN 154806 | 1506 | None | 0 | Human | Binding | pKi | = | - | 7.20 | -19 | 6 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/12616335 | |
[D-Tyr8]CYN 154806 | 1506 | None | 0 | Mouse | Binding | pKi | = | - | 7.05 | -28 | 6 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/10818261 | |
[L-Tyr8]CYN 154806 | 2375 | None | 0 | Human | Binding | pKi | = | - | 8.20 | -1 | 6 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/12616335 | |
[L-Tyr8]CYN 154806 | 2375 | None | 0 | Mouse | Binding | pKi | = | - | 6.70 | -35 | 6 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/10818261 | |
AC-178,335 | 234 | None | 0 | Rat | Binding | pKi | = | - | 6.60 | -1 | 2 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9804621 | |
astemizole | 505 | None | 55 | Human | Binding | pKi | = | 5.39 | 8.27 | -85 | 48 | Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells | Drug Central | 458.2 | 8 | 1 | 5 | 5.35 | COc1ccc(CCN2CCC(Nc3nc4ccccc4n3Cc3ccc(F)cc3)CC2)cc1 | - | |
astemizole | 505 | None | 55 | Human | Binding | Ki | = | 4070.00 | 5.39 | -85 | 48 | Displacement of [125I]11-Tyr somatostatin-14 from human SST5R expressed in CHO cells | ChEMBL | 458.2 | 8 | 1 | 5 | 5.35 | COc1ccc(CCN2CCC(Nc3nc4ccccc4n3Cc3ccc(F)cc3)CC2)cc1 | https://dx.doi.org/10.1021/jm701143p | |
astemizole | 505 | None | 55 | Human | Binding | Ki | = | 4070.00 | 5.39 | -85 | 48 | Displacement of SST14 from human recombinant SST5 receptor expressed in CHO cells by radioligand binding assay | ChEMBL | 458.2 | 8 | 1 | 5 | 5.35 | COc1ccc(CCN2CCC(Nc3nc4ccccc4n3Cc3ccc(F)cc3)CC2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2009.09.024 | |
BIM 23023 | 637 | None | 0 | Human | Binding | pKi | = | - | 8.90 | -3 | 8 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9600011 | |
BIM 23023 | 637 | None | 0 | Human | Binding | pKi | = | - | 8.90 | -3 | 8 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/7988476 | |
BIM 23023 | 637 | None | 0 | Rat | Binding | pKi | = | - | 7.80 | -39 | 8 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9600011 | |
BIM 23030 | 639 | None | 0 | Human | Binding | pKi | = | - | 6.50 | -19 | 5 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/10598788 | |
BIM 23030 | 639 | None | 0 | Mouse | Binding | pKi | = | - | 7.55 | -1 | 5 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/10818261 | |
BIM 23050 | 641 | None | 0 | Human | Binding | pKi | = | - | 8.80 | 10 | 4 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/7988476 | |
BIM 23052 | 642 | None | 0 | Human | Binding | pKi | = | - | 8.50 | -3 | 9 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9650799 | |
BIM 23052 | 642 | None | 0 | Human | Binding | pKi | = | - | 8.50 | -3 | 9 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/10598788 | |
BIM 23052 | 642 | None | 0 | Human | Binding | pKi | = | - | 8.50 | -3 | 9 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9600011 | |
BIM 23052 | 642 | None | 0 | Human | Binding | pKi | = | - | 8.50 | -3 | 9 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9652348 | |
BIM 23052 | 642 | None | 0 | Rat | Binding | pKi | = | - | 8.60 | -2 | 9 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9600011 | |
BIM 23056 | 643 | None | 0 | Human | Binding | pKi | = | - | 7.85 | -1 | 7 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | - |
Showing 1 to 20 of 1,121 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 | |
BIM 23197 | 650 | None | 0 | Human | Functional | pIC50 | = | - | 8.00 | -50 | 3 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9045884 | |
BIM 23454 | 654 | None | 0 | Human | Functional | pIC50 | = | - | 6.90 | -3 | 5 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/11897676 | |
BIM 23627 | 655 | None | 0 | Human | Functional | pIC50 | = | - | 7.10 | -12 | 5 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/11897676 | |
BOC-ATE | 700 | None | 0 | Human | Functional | pIC50 | = | - | 8.40 | -5 | 3 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/15709181 | |
CHEMBL1079874 | 5958 | None | 0 | Human | Functional | IC50 | = | 72.00 | 7.14 | - | 4 | Antagonist activity at human SST5 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP release by TR-FRET assay | ChEMBL | 457.2 | 9 | 2 | 7 | 4.54 | CCOc1cc(CN2CCC(Nc3nc4ccc(C(=O)O)cc4o3)CC2)cc(OCC)c1F | https://dx.doi.org/10.1016/j.bmcl.2009.09.024 | |
CHEMBL1080586 | 6067 | None | 0 | Human | Functional | IC50 | = | 98.00 | 7.01 | - | 4 | Antagonist activity at human SST5 receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP release by TR-FRET assay | ChEMBL | 429.1 | 7 | 2 | 6 | 4.66 | CCOc1cc(CN2CCC(Nc3nc4ccc(C(=O)O)cc4o3)CC2)ccc1Cl | https://dx.doi.org/10.1016/j.bmcl.2009.09.024 | |
CHEMBL1210207 | 15185 | None | 0 | Human | Functional | IC50 | = | 3.10 | 8.51 | -1 | 2 | Antagonist activity at human SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assay | ChEMBL | 491.3 | 9 | 1 | 5 | 5.39 | CCOc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)cc(OCC)c1-c1ccc(F)cc1 | https://dx.doi.org/10.1021/acsmedchemlett.8b00305 | |
CHEMBL1210207 | 15185 | None | 0 | Mouse | Functional | IC50 | = | 2.70 | 8.57 | 1 | 2 | Antagonist activity at mouse SSTR5 expressed in CHO-K1 cell membranes assessed as reduction in SST-28-induced inhibition of forskolin-stimulated cAMP accumulation by LANCE assay | ChEMBL | 491.3 | 9 | 1 | 5 | 5.39 | CCOc1cc(CN2CCC(NC(=O)c3cncc(C)c3)CC2)cc(OCC)c1-c1ccc(F)cc1 | https://dx.doi.org/10.1021/acsmedchemlett.8b00305 | |
CHEMBL165402 | 57445 | None | 0 | Human | Functional | EC50 | = | 1600.00 | 5.80 | - | 4 | Agonist activity on human somatostatin receptor 5 | ChEMBL | 475.2 | 7 | 2 | 6 | 5.23 | CC(C)(C(=O)NC1CCCCC1)c1cn2cc(-c3csc4ccccc34)nc(CCCN)c2n1 | https://dx.doi.org/10.1016/s0960-894x(01)00051-8 | |
CHEMBL187768 | 67212 | None | 0 | Human | Functional | EC50 | = | 34.00 | 7.47 | -1 | 5 | Inhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst5 receptor | ChEMBL | 456.2 | 9 | 2 | 6 | 5.36 | Cc1cccc2c(CCSc3nnc(-c4ccc5ccccc5n4)n3CCCCN)c[nH]c12 | https://dx.doi.org/10.1016/j.bmcl.2005.05.061 | |
CHEMBL189554 | 67540 | None | 0 | Human | Functional | EC50 | = | 52.00 | 7.28 | -8 | 2 | Inhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst5 receptor | ChEMBL | 476.2 | 9 | 2 | 6 | 5.70 | NCCCCn1c(SCCc2c[nH]c3ccc(Cl)cc23)nnc1-c1ccc2ccccc2n1 | https://dx.doi.org/10.1016/j.bmcl.2005.05.061 | |
CHEMBL227212 | 85541 | None | 0 | Human | Functional | IC50 | = | 1.20 | 8.92 | -1 | 5 | Agonist activity at human SST5 receptor expressed in CHOK1 cells assessed as effect on forskolin-induced cAMP production | ChEMBL | 551.3 | 11 | 4 | 4 | 3.59 | NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O | https://dx.doi.org/10.1021/jm070246f | |
CHEMBL227212 | 85541 | None | 0 | Human | Functional | EC50 | = | 13.00 | 7.89 | -1 | 5 | Agonist activity at human SST5 receptor expressed in CHOK1 cells assessed as effect on forskolin-induced cAMP production | ChEMBL | 551.3 | 11 | 4 | 4 | 3.59 | NCCCC[C@@H](C(=O)NCc1ccccc1)N1Cc2[nH]c3ccccc3c2C[C@@H](NC(=O)Cc2ccccc2)C1=O | https://dx.doi.org/10.1021/jm070246f | |
CHEMBL236587 | 89180 | None | 0 | Human | Functional | IC50 | = | 740.00 | 6.13 | - | 6 | Antagonist activity at human SST5R expressed in CHO cells assessed as reversal of somatostatin-14 induced cAMP response | ChEMBL | 381.2 | 7 | 1 | 6 | 4.31 | CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)ccc1OC | https://dx.doi.org/10.1021/jm701143p | |
CHEMBL363092 | 124111 | None | 0 | Human | Functional | EC50 | = | 44.00 | 7.36 | -3 | 5 | Inhibition of forskolin-induced cAMP accumulation in CHO-K1 cells expressing human sst5 receptor | ChEMBL | 460.2 | 9 | 2 | 6 | 5.19 | NCCCCn1c(SCCc2c[nH]c3cc(F)ccc23)nnc1-c1ccc2ccccc2n1 | https://dx.doi.org/10.1016/j.bmcl.2005.05.061 | |
CHEMBL3665800 | 128474 | None | 0 | Human | Functional | IC50 | = | 1.50 | 8.82 | -3 | 2 | Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay | ChEMBL | 548.2 | 9 | 1 | 6 | 5.98 | CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 | https://dx.doi.org/10.1021/acsmedchemlett.8b00306 | |
CHEMBL3665800 | 128474 | None | 0 | Mouse | Functional | IC50 | = | 0.30 | 9.52 | 3 | 2 | Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay | ChEMBL | 548.2 | 9 | 1 | 6 | 5.98 | CCOc1cc(CN2CCC3(CC2)CN(c2ccc(C(=O)O)cc2)C(=O)O3)cc(OCC)c1-c1ccc(F)cc1 | https://dx.doi.org/10.1021/acsmedchemlett.8b00306 | |
CHEMBL3670722 | 129287 | None | 0 | Human | Functional | IC50 | = | 1.10 | 8.96 | 15 | 2 | Antagonist activity at human SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay | ChEMBL | 450.2 | 4 | 1 | 5 | 4.44 | CC1(C)CCOc2ccc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)cc21 | https://dx.doi.org/10.1021/acsmedchemlett.8b00306 | |
CHEMBL3670722 | 129287 | None | 0 | Mouse | Functional | IC50 | = | 21.00 | 7.68 | -15 | 2 | Antagonist activity at mouse SSR5 expressed in CHOK1 cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition measured after 1 hr by LANCE assay | ChEMBL | 450.2 | 4 | 1 | 5 | 4.44 | CC1(C)CCOc2ccc(CN3CCC4(CC3)CN(c3ccc(C(=O)O)cc3)C(=O)O4)cc21 | https://dx.doi.org/10.1021/acsmedchemlett.8b00306 | |
CHEMBL4059929 | 155912 | None | 0 | Human | Functional | IC50 | = | 6.70 | 8.17 | 5 | 2 | Antagonist activity at human SSTR5 expressed in CHO cells assessed as inhibition of SST14-induced forskolin-stimulated intracellular cAMP level incubated for 15 mins followed by forskolin stimulation for 30 mins by HTRF assay | ChEMBL | 535.3 | 7 | 1 | 6 | 5.55 | CCOc1c(CN2CC3(CC(N4CCC(C)(C(=O)O)CC4)=NO3)C2)cc(C2CC2)c(-c2ccc(F)cc2)c1C | https://dx.doi.org/10.1016/j.bmc.2017.06.003 |
Showing 1 to 20 of 246 entries