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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 | = | - | 5.15 | -2238 | 6 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/12616335 | |
[L-Tyr8]CYN 154806 | 2375 | None | 0 | Human | Binding | pKi | = | - | 5.80 | -281 | 6 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/12616335 | |
ARSENIC TRIOXIDE | 197249 | None | 1 | Rat | Binding | Kd | = | 52.48 | 7.28 | 478 | 2 | Displacement of [125I]SRIF14 from rat sst1 receptor from rat brain cortex membrane | ChEMBL | 197.8 | 1 | 0 | 3 | -2.19 | O=[As][As+](=O)[O-] | https://dx.doi.org/10.1016/j.bmcl.2007.04.078 | |
BIM 23052 | 642 | None | 0 | Human | Binding | pKi | None | - | 8.40 | -4 | 9 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/8769372 | |
BIM 23052 | 642 | None | 0 | Human | Binding | pKi | None | - | 8.40 | -4 | 9 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9650799 | |
BIM 23052 | 642 | None | 0 | Human | Binding | pKi | None | - | 8.40 | -4 | 9 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/10598788 | |
BIM 23268 | 218833 | UNDEFINED | 0 | Human | Binding | pKi | = | 18.40 | 7.74 | -112 | 9 | - | PDSP KiDatabase | 1077.5 | 14 | 12 | 13 | 0.55 | CC(O)C1NC(=O)C(CCCCN)NC(=O)C(Cc2c[nH]c3ccccc23)NC(=O)C(Cc2ccccc2)NC(=O)C(Cc2ccccc2)NC(=O)C(N)CSSCC(C(N)=O)NC(=O)C(Cc2ccccc2)NC1=O | - | |
BIM 23268 | 218833 | 125I-SOMATOSTATIN | 0 | Human | Binding | pKi | = | 582.00 | 6.24 | -112 | 9 | - | PDSP KiDatabase | 1077.5 | 14 | 12 | 13 | 0.55 | CC(O)C1NC(=O)C(CCCCN)NC(=O)C(Cc2c[nH]c3ccccc23)NC(=O)C(Cc2ccccc2)NC(=O)C(Cc2ccccc2)NC(=O)C(N)CSSCC(C(N)=O)NC(=O)C(Cc2ccccc2)NC1=O | - | |
BIM 23268 | 218833 | 125I-Tyr11-somatostatin-14 | 0 | Human | Binding | pKi | = | 18.40 | 7.74 | -112 | 9 | - | PDSP KiDatabase | 1077.5 | 14 | 12 | 13 | 0.55 | CC(O)C1NC(=O)C(CCCCN)NC(=O)C(Cc2c[nH]c3ccccc23)NC(=O)C(Cc2ccccc2)NC(=O)C(Cc2ccccc2)NC(=O)C(N)CSSCC(C(N)=O)NC(=O)C(Cc2ccccc2)NC1=O | - | |
BN-81,644 | 697 | None | 5 | Human | Binding | Ki | = | 3700.00 | 5.43 | -5888 | 4 | Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-1) subtype | ChEMBL | 426.3 | 8 | 3 | 2 | 7.02 | CCCCC1(CCCC)N[C@@H](c2ncc(-c3ccccc3)[nH]2)Cc2c1[nH]c1ccccc21 | https://dx.doi.org/10.1021/jm0108449 | |
CGP 23996 | 891 | None | 0 | Human | Binding | pKi | = | - | 8.35 | -5 | 6 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/8769372 | |
CGP 23996 | 891 | None | 0 | Human | Binding | pKi | = | - | 8.35 | -5 | 6 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9650799 | |
CGP 23996 | 891 | None | 0 | Human | Binding | pKi | = | - | 8.35 | -5 | 6 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/10598788 | |
CHEMBL102892 | 4627 | None | 0 | Human | Binding | Ki | = | 1800.00 | 5.75 | -1047 | 2 | Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-1) subtype | ChEMBL | 396.2 | 3 | 3 | 2 | 6.07 | c1ccc(-c2c[nH]c(C3Cc4c([nH]c5ccccc45)C(C4CCCCC4)N3)n2)cc1 | https://dx.doi.org/10.1021/jm0108449 | |
CHEMBL1076620 | 5539 | None | 0 | Human | Binding | Kd | = | 436.52 | 6.36 | -194 | 2 | Binding affinity to human SST1 receptor | ChEMBL | 620.3 | 9 | 0 | 9 | 4.43 | COC(=O)c1cc(C[C@@H](C)CN2C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)[C@H]3CCCC[C@H]3C2)cc(C(=O)OC)c1 | https://dx.doi.org/10.1016/j.bmcl.2010.01.063 | |
CHEMBL1076621 | 5540 | None | 0 | Human | Binding | Kd | = | 933.25 | 6.03 | -758 | 2 | Binding affinity to human SST1 receptor | ChEMBL | 620.3 | 9 | 0 | 9 | 4.43 | COC(=O)c1cc(C[C@H](C)CN2C[C@@H](C(=O)N3CCN(c4ccc([N+](=O)[O-])cc4)CC3)[C@H]3CCCC[C@H]3C2)cc(C(=O)OC)c1 | https://dx.doi.org/10.1016/j.bmcl.2010.01.063 | |
CHEMBL1076622 | 5541 | None | 0 | Human | Binding | Kd | = | 1380.38 | 5.86 | -407 | 7 | Binding affinity to human SST1 receptor | ChEMBL | 550.3 | 6 | 0 | 5 | 5.68 | Cc1nc2cc(C[C@H](C)CN3C[C@@H](C(=O)N4CCN(c5ccc(F)c(F)c5)CC4)[C@H]4CCCC[C@H]4C3)ccc2o1 | https://dx.doi.org/10.1016/j.bmcl.2010.01.063 | |
CHEMBL1076622 | 5541 | None | 0 | Rat | Binding | Kd | = | 457.09 | 6.34 | -134 | 7 | Displacement of [125I]SRIF-14 from rat cortex membrane SST1 receptor | ChEMBL | 550.3 | 6 | 0 | 5 | 5.68 | Cc1nc2cc(C[C@H](C)CN3C[C@@H](C(=O)N4CCN(c5ccc(F)c(F)c5)CC4)[C@H]4CCCC[C@H]4C3)ccc2o1 | https://dx.doi.org/10.1016/j.bmcl.2010.01.063 | |
CHEMBL1076627 | 5542 | None | 0 | Human | Binding | Kd | = | 39.81 | 7.40 | 2 | 2 | Binding affinity to human SST1 receptor | ChEMBL | 549.3 | 6 | 0 | 5 | 5.19 | Cc1cn2cc(C[C@H](C)CN3C[C@@H](C(=O)N4CCN(c5ccc(F)c(F)c5)CC4)[C@H]4CCCC[C@H]4C3)ccc2n1 | https://dx.doi.org/10.1016/j.bmcl.2010.01.063 | |
CHEMBL1076652 | 5544 | None | 0 | Human | Binding | Kd | = | 489.78 | 6.31 | -3 | 2 | Binding affinity to human SST1 receptor | ChEMBL | 548.3 | 7 | 0 | 7 | 4.73 | CC(Cc1ccc2c(c1)OCO2)CN1C[C@H](C(=O)N2CCN(c3ccc([N+](=O)[O-])cc3)CC2)C[C@@H]2CCCC[C@@H]21 | https://dx.doi.org/10.1016/j.bmcl.2010.01.063 |
Showing 1 to 20 of 804 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 23050 | 641 | None | 0 | Human | Functional | pIC50 | = | - | 6.40 | -79 | 4 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/8100350 | |
BIM 23454 | 654 | None | 0 | Human | Functional | pIC50 | None | - | 6.00 | -31 | 5 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/11897676 | |
BIM 23627 | 655 | None | 0 | Human | Functional | pIC50 | = | - | 5.60 | -398 | 5 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/11897676 | |
CH 275 | 906 | None | 0 | Human | Functional | pIC50 | None | - | 8.50 | 15 | 2 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9600011 | |
CH 275 | 906 | None | 0 | Rat | Functional | pIC50 | = | - | 7.30 | -15 | 2 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9166718 | |
CHEMBL4277106 | 166509 | None | 0 | Human | Functional | IC50 | = | 6000.00 | 5.22 | -1778 | 3 | Antagonist activity at human SSTR1 expressed in CHO-K1 cell membranes | ChEMBL | 559.2 | 10 | 2 | 7 | 6.59 | CCOc1cc(CN2CC[C@H]3C(Nc4nc5ccc(C(=O)O)cc5o4)CC[C@H]32)cc(OCC)c1-c1ccc(F)cc1 | https://dx.doi.org/10.1021/acsmedchemlett.8b00305 | |
CHEMBL553655 | 197965 | None | 0 | Human | Functional | EC50 | = | 3.90 | 8.41 | 48 | 3 | Agonist activity at human sst1 receptor expressed in Chinese hamster CCL39 cells by luciferase reporter gene assay relative to somatostatin-14 | ChEMBL | 1074.4 | 15 | 10 | 13 | 1.59 | CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 | https://dx.doi.org/10.1021/jm801314f | |
CHEMBL556949 | 218226 | None | 0 | Human | Functional | EC50 | = | 33.00 | 7.48 | - | 1 | Agonist activity at human sst1 receptor expressed in Chinese hamster CCL39 cells by luciferase reporter gene assay relative to somatostatin-14 | ChEMBL | - | - | - | - | - | CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@@H](N)Cc3ccc(O)cc3)CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@H]([C@@H](C)O)NC2=O)cc1 | https://dx.doi.org/10.1021/jm801314f | |
CHEMBL558161 | 198273 | None | 0 | Human | Functional | EC50 | = | 0.37 | 9.43 | 100 | 3 | Agonist activity at human sst1 receptor expressed in Chinese hamster CCL39 cells by luciferase reporter gene assay relative to somatostatin-14 | ChEMBL | 1237.5 | 19 | 12 | 15 | 2.03 | CC(C)NCc1ccc(C[C@@H]2NC(=O)[C@@H](N(C)C(=O)c3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccccc3)NC(=O)[C@@H](NC(=O)[C@H](N)Cc3ccc(O)cc3)CSSC[C@@H](C(=O)N[C@H](C(N)=O)[C@@H](C)O)NC(=O)[C@H](Cc3ccccc3)NC2=O)cc1 | https://dx.doi.org/10.1021/jm801314f | |
CHEMBL563125 | 218236 | None | 0 | Human | Functional | EC50 | = | 0.93 | 9.03 | - | 1 | Agonist activity at human sst1 receptor expressed in Chinese hamster CCL39 cells by luciferase reporter gene assay relative to somatostatin-14 | ChEMBL | - | - | - | - | - | C[C@H](N)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](c2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC1=O | https://dx.doi.org/10.1021/jm801314f | |
cyclo(7-12) Des-AA1,2,5-[Glu7,D-Trp8,IAmp9,m-I-Tyr11,hhLys12]SRIF | 1281 | None | 0 | Human | Functional | pIC50 | = | - | 8.20 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/15658865 | |
Des-AA1,2,5,12,13-[D-Trp8]SRIF | 1373 | None | 0 | Human | Functional | pIC50 | = | - | 8.30 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/15658865 | |
Des-AA1,5-[Tyr2,D-Trp8,IAmp9]SRIF | 1374 | None | 0 | Human | Functional | pIC50 | = | - | 7.80 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/15658865 | |
Des-AA5-[D-Trp8]SRIF | 1375 | None | 0 | Human | Functional | pIC50 | = | - | 9.00 | 1 | 4 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/15658864 | |
Des-Ala1,2,5-[D-Trp8,IAmp9]SRIF | 1376 | None | 0 | Human | Functional | pIC50 | = | - | 7.50 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/15658864 | |
KE 108 | 2180 | None | 0 | Human | Functional | pIC50 | = | - | 8.60 | -3 | 6 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/12450568 | |
pasireotide | 3007 | None | 26 | Human | Functional | pIC50 | = | - | 8.00 | -63 | 22 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/15477717 | |
pasireotide | 220222 | None | 0 | Human | Functional | pIC50 | = | 8.00 | 8.10 | 1 | 5 | None | Drug Central | 1046.5 | 17 | 9 | 11 | 3.37 | NCCCC[C@@H]1NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)C(c2ccccc2)NC(=O)[C@@H]2C[C@@H](OC(=O)NCCN)CN2C(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](Cc2ccc(OCc3ccccc3)cc2)NC1=O | - | |
SRIF-14 | 3675 | None | 0 | Rat | Functional | pIC50 | None | - | 8.40 | -50 | 13 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9166718 |
Showing 1 to 19 of 19 entries