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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 | |
1-(benzo[d]thiazol-2-yl)-N-(3-ethoxy-4-methoxyphenyl)piperidin-4-amine | 220110 | UNDEFINED | 0 | Human | Binding | pKi | = | 10000.00 | 5.00 | -1 | 3 | - | PDSP KiDatabase | 383.2 | 6 | 1 | 6 | 4.78 | CCOc1cc(NC2CCN(c3nc4ccccc4s3)CC2)ccc1OC | - | |
1-(benzo[d]thiazol-2-ylmethyl)-N-(3-ethoxy-4-methoxyphenyl)piperidin-4-amine | 220111 | UNDEFINED | 0 | Human | Binding | pKi | = | 10000.00 | 5.00 | -1 | 3 | - | PDSP KiDatabase | 397.2 | 7 | 1 | 6 | 4.78 | CCOc1cc(NC2CCN(Cc3nc4ccccc4s3)CC2)ccc1OC | - | |
2-(4-((4-(benzo[d]oxazol-2-ylamino)piperidin-1-yl)methyl)-2-ethoxy-5-fluorophenoxy)ethanol | 220122 | UNDEFINED | 0 | Human | Binding | pKi | = | 10000.00 | 5.00 | -1 | 3 | - | PDSP KiDatabase | 429.2 | 9 | 2 | 7 | 3.81 | CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)c(F)cc1OCCO | - | |
[D-Tyr8]CYN 154806 | 1506 | None | 0 | Human | Binding | pKi | = | - | 6.45 | -112 | 6 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/10818261 | |
[L-Tyr8]CYN 154806 | 2375 | None | 0 | Human | Binding | pKi | = | - | 6.50 | -56 | 6 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/10818261 | |
ACQ090 | 266 | None | 0 | Human | Binding | pKi | = | - | 7.90 | - | 1 | Unclassified | Guide to Pharmacology | 526.3 | 7 | 0 | 5 | 4.63 | COc1ccc(CC(C)CN2C[C@@H](C(=O)N3CCN(c4ccc(F)c(F)c4)CC3)[C@H]3CCCC[C@H]3C2)cn1 | - | |
astemizole | 505 | UNDEFINED | 55 | Human | Binding | pKi | = | 10000.00 | 5.00 | -5754 | 48 | - | PDSP KiDatabase | 458.2 | 8 | 1 | 5 | 5.35 | COc1ccc(CCN2CCC(Nc3nc4ccccc4n3Cc3ccc(F)cc3)CC2)cc1 | - | |
BIM 23023 | 637 | None | 0 | Human | Binding | pKi | = | - | 8.10 | -19 | 8 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/7988476 | |
BIM 23023 | 637 | None | 0 | Rat | Binding | pKi | = | - | 7.00 | -251 | 8 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9600011 | |
BIM 23030 | 639 | None | 0 | Human | Binding | pKi | = | - | 7.50 | -1 | 5 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9650799 | |
BIM 23030 | 639 | None | 0 | Human | Binding | pKi | = | - | 7.50 | -1 | 5 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/10598788 | |
BIM 23034 | 640 | None | 0 | Human | Binding | pKi | = | - | 8.10 | -3 | 4 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/7988476 | |
BIM 23050 | 641 | None | 0 | Human | Binding | pKi | = | - | 7.80 | -10 | 4 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/7988476 | |
BIM 23052 | 642 | None | 0 | Human | Binding | pKi | = | - | 9.05 | 2 | 9 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/8769372 | |
BIM 23052 | 642 | None | 0 | Human | Binding | pKi | = | - | 9.05 | 2 | 9 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9650799 | |
BIM 23052 | 642 | None | 0 | Human | Binding | pKi | = | - | 9.05 | 2 | 9 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/10598788 | |
BIM 23052 | 642 | None | 0 | Rat | Binding | pKi | = | - | 8.50 | -3 | 9 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9600011 | |
BIM 23056 | 643 | None | 0 | Human | Binding | pKi | = | - | 7.05 | -4 | 7 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9650799 | |
BIM 23056 | 643 | None | 0 | Human | Binding | pKi | = | - | 7.05 | -4 | 7 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/10598788 | |
BIM 23058 | 644 | None | 0 | Human | Binding | pKi | = | - | 8.80 | - | 2 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/7988476 |
Showing 1 to 20 of 1,068 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 23023 | 637 | None | 0 | Mouse | Functional | pIC50 | = | - | 7.90 | - | 8 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/8100350 | |
BIM 23034 | 640 | None | 0 | Mouse | Functional | pIC50 | = | - | 7.20 | -31622 | 4 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/8100350 | |
BIM 23050 | 641 | None | 0 | Mouse | Functional | pIC50 | = | - | 8.30 | 79 | 4 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/8100350 | |
BIM 23052 | 642 | None | 0 | Mouse | Functional | pIC50 | = | - | 9.40 | 19 | 9 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/8100350 | |
BIM 23056 | 643 | None | 0 | Mouse | Functional | pIC50 | = | - | 10.70 | 15848 | 7 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/8100350 | |
BIM 23056 | 643 | None | 0 | Rat | Functional | pIC50 | = | - | 6.50 | -15848 | 7 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9166718 | |
BIM 23058 | 644 | None | 0 | Mouse | Functional | pIC50 | = | - | 10.40 | - | 2 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/8100350 | |
BIM 23059 | 645 | None | 0 | Mouse | Functional | pIC50 | = | - | 8.20 | -794 | 4 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/8100350 | |
BIM 23066 | 647 | None | 0 | Mouse | Functional | pIC50 | = | - | 9.00 | 3 | 2 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/8100350 | |
BIM 23068 | 648 | None | 0 | Mouse | Functional | pIC50 | = | - | 9.10 | -5 | 6 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/8100350 | |
BIM 23197 | 650 | None | 0 | Human | Functional | pIC50 | = | - | 7.60 | -125 | 3 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9045884 | |
BIM 23454 | 654 | None | 0 | Human | Functional | pIC50 | = | - | 7.30 | -1 | 5 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/11897676 | |
BIM 23627 | 655 | None | 0 | Human | Functional | pIC50 | = | - | 7.40 | -6 | 5 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/11897676 | |
BN-81,644 | 697 | None | 5 | Human | Functional | IC50 | = | 2.70 | 8.57 | - | 4 | Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor. | 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 | |
BOC-ATE | 700 | None | 0 | Human | Functional | pIC50 | = | - | 7.50 | -39 | 3 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/15709181 | |
CHEMBL102892 | 4627 | None | 0 | Human | Functional | IC50 | = | 19.00 | 7.72 | - | 2 | Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor. | 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 | |
CHEMBL1237140 | 16536 | None | 0 | Human | Functional | IC50 | = | 2.70 | 8.57 | - | 3 | Antagonist activity at human SST3 expressed in CHO-K1 cells assessed as inhibition of SRIF-14-induced foreskin-stimulated cAMP accumulation after 45 mins by TR-FRET assay | ChEMBL | 426.3 | 8 | 3 | 2 | 7.02 | CCCCC1(CCCC)N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 | https://dx.doi.org/10.1021/ml500079u | |
CHEMBL1237140 | 16536 | None | 0 | Human | Functional | IC50 | = | 6.80 | 8.17 | - | 3 | Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor. | ChEMBL | 426.3 | 8 | 3 | 2 | 7.02 | CCCCC1(CCCC)N[C@H](c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccccc21 | https://dx.doi.org/10.1021/jm0108449 | |
CHEMBL173778 | 60087 | None | 0 | Human | Functional | IC50 | = | 450.00 | 6.35 | - | 1 | Inhibitory concentration required to inhibit SRIF-14 induced reduction of cAMP in CHO-K1 cells expressing the human sst3 receptor. | ChEMBL | 468.3 | 10 | 3 | 2 | 8.11 | CCCCCC1(CCCCC)NC(c2nc(-c3ccccc3)c[nH]2)Cc2c1[nH]c1ccc(C)cc21 | https://dx.doi.org/10.1021/jm0108449 | |
CHEMBL1823873 | 211491 | None | 10 | Human | Functional | EC50 | = | 0.63 | 9.20 | -1 | 5 | Agonist activity at human sst3 receptor expressed in CCL39 cells after 5 hrs by luciferase reporter gene assay | 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](Cc2c[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/jm200307v |
Showing 1 to 20 of 269 entries