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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 | |
(+)-ADTN | 297 | None | 18 | Human | Binding | pKi | None | - | 6.00 | -588 | 7 | Unclassified | Guide to Pharmacology | 179.1 | 0 | 3 | 3 | 0.91 | NC1CCc2cc(O)c(O)cc2C1 | https://pubmed.ncbi.nlm.nih.gov/1826762 | |
(+)-butaclamol | 746 | 3H-SCH23390 | 9 | Human | Binding | pKi | = | 27.00 | 7.57 | -61 | 25 | - | PDSP KiDatabase | 361.2 | 0 | 1 | 2 | 4.84 | CC(C)(C)[C@]1(O)CCN2C[C@H]3c4ccccc4CCc4cccc(c43)[C@@H]2C1 | - | |
(+)-butaclamol | 746 | None | 9 | Human | Binding | pKi | None | - | 7.60 | -61 | 25 | Unclassified | Guide to Pharmacology | 361.2 | 0 | 1 | 2 | 4.84 | CC(C)(C)[C@]1(O)CCN2C[C@H]3c4ccccc4CCc4cccc(c43)[C@@H]2C1 | https://pubmed.ncbi.nlm.nih.gov/1826762 | |
(-)-stepholidine | 3691 | None | 40 | Human | Binding | Ki | = | 4.40 | 8.36 | 1 | 35 | Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in CHO cells by scintillation counting | ChEMBL | 327.1 | 2 | 2 | 5 | 2.77 | COc1cc2c(cc1O)[C@@H]1Cc3ccc(O)c(OC)c3CN1CC2 | https://dx.doi.org/10.1016/j.bmc.2009.08.028 | |
(-)-stepholidine | 3691 | 3H-SCH23390 | 40 | Human | Binding | pKi | = | 4.40 | 8.36 | 1 | 35 | - | PDSP KiDatabase | 327.1 | 2 | 2 | 5 | 2.77 | COc1cc2c(cc1O)[C@@H]1Cc3ccc(O)c(OC)c3CN1CC2 | - | |
(1R,2S)-PHENYLPROPANOLAMINE | 27120 | 3H-SCH23390 | 13 | Human | Binding | pKi | = | 10000.00 | 5.00 | -38 | 42 | - | PDSP KiDatabase | 151.1 | 2 | 2 | 2 | 1.07 | C[C@H](N)[C@H](O)c1ccccc1 | - | |
(R)-SKF-38393 | 91633 | None | 9 | Human | Binding | Ki | = | 245.47 | 6.61 | 3 | 6 | Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin) | ChEMBL | 255.1 | 1 | 3 | 3 | 2.38 | Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 | https://dx.doi.org/10.1016/j.bmcl.2013.12.024 | |
(R)-SKF-38393 | 91633 | None | 9 | Human | Binding | Ki | = | 0.50 | 9.30 | 3 | 6 | Agonist activity at dopamine D5 receptor (unknown origin) | ChEMBL | 255.1 | 1 | 3 | 3 | 2.38 | Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 | https://dx.doi.org/10.1016/j.bmcl.2020.127305 | |
(R)-SKF-38393 | 91633 | None | 9 | Human | Binding | Ki | = | 247.00 | 6.61 | 3 | 6 | Displacement of [3H]SCH23390 from dopamine D5 receptor (unknown origin) | ChEMBL | 255.1 | 1 | 3 | 3 | 2.38 | Oc1cc2c(cc1O)[C@@H](c1ccccc1)CNCC2 | https://dx.doi.org/10.1016/j.bmcl.2013.12.024 | |
2-(4'-Methylaminophenyl)Benzothiazole | 220178 | 3H-SCH23390 | 0 | Human | Binding | pKi | = | 13.00 | 7.89 | -6 | 7 | - | PDSP KiDatabase | 268.1 | 3 | 1 | 5 | 4.75 | CNc1ccc(N=Nc2ccc3ncsc3c2)cc1 | - | |
5-hydroxytryptamine | 139 | None | 45 | Human | Binding | pKi | None | - | 5.50 | -7244 | 61 | Unclassified | Guide to Pharmacology | 176.1 | 2 | 3 | 2 | 1.38 | NCCc1c[nH]c2ccc(O)cc12 | https://pubmed.ncbi.nlm.nih.gov/1826762 | |
5-hydroxytryptamine | 139 | 3H-SCH23390 | 45 | Human | Binding | pKi | = | 3000.00 | 5.52 | -7244 | 61 | - | PDSP KiDatabase | 176.1 | 2 | 3 | 2 | 1.38 | NCCc1c[nH]c2ccc(O)cc12 | - | |
A77636 | 208 | None | 8 | Human | Binding | Ki | = | 3.02 | 8.52 | 1 | 27 | PDSP Secondary Binding target: DRD5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | ChEMBL | 329.2 | 2 | 3 | 4 | 3.25 | NC[C@@H]1O[C@H](C23CC4CC(CC(C4)C2)C3)Cc2c1ccc(O)c2O | https://dx.doi.org/10.6019/CHEMBL5442175 | |
ABT-594 | 219818 | 3H-SCH23390 | 0 | Human | Binding | pKi | = | 1000.00 | 6.00 | -2 | 37 | - | PDSP KiDatabase | 198.1 | 3 | 1 | 3 | 1.48 | Clc1ccc(OCC2CCN2)cn1 | - | |
ADTN, (+) | 218719 | 3H-SCH23390 | 0 | Human | Binding | pKi | = | 909.00 | 6.04 | -2 | 4 | - | PDSP KiDatabase | 226.2 | 0 | 2 | 2 | 1.35 | O=C1CCCCCNC(=O)CCCCCN1 | - | |
AMENTOFLAVONE | 205483 | 3H-SCH23390 | 63 | Human | Binding | pKi | = | 10000.00 | 5.00 | -275 | 33 | - | PDSP KiDatabase | 538.1 | 3 | 6 | 10 | 5.13 | O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 | - | |
amisulpride | 400 | 3H-SCH23390 | 72 | Human | Binding | pKi | = | 10000.00 | 5.00 | -4365 | 53 | - | PDSP KiDatabase | 369.2 | 7 | 2 | 6 | 1.28 | CCN1CCCC1CNC(=O)c1cc(S(=O)(=O)CC)c(N)cc1OC | - | |
amitriptyline | 401 | UNDEFINED | 38 | Human | Binding | pKi | = | 170.00 | 6.77 | -112 | 51 | - | PDSP KiDatabase | 277.2 | 3 | 0 | 1 | 4.17 | CN(C)CCC=C1c2ccccc2CCc2ccccc21 | - | |
amitriptyline | 401 | None | 38 | Human | Binding | pKi | = | 6.77 | 8.17 | -112 | 51 | None | Drug Central | 277.2 | 3 | 0 | 1 | 4.17 | CN(C)CCC=C1c2ccccc2CCc2ccccc21 | - | |
amitriptyline | 401 | None | 38 | Human | Binding | Ki | = | 170.00 | 6.77 | -112 | 51 | Displacement of [3H]SCH23390 from human dopamine D5 receptor expressed in HEK cells | ChEMBL | 277.2 | 3 | 0 | 1 | 4.17 | CN(C)CCC=C1c2ccccc2CCc2ccccc21 | https://dx.doi.org/10.1016/j.bmcl.2008.09.012 |
Showing 1 to 20 of 717 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 | |
A68930 | 205 | None | 17 | Human | Functional | pEC50 | = | - | 6.60 | -128 | 5 | Unclassified | Guide to Pharmacology | 271.1 | 2 | 3 | 4 | 2.41 | NC[C@@H]1O[C@H](c2ccccc2)Cc2c1ccc(O)c2O | https://pubmed.ncbi.nlm.nih.gov/16318870 | |
CHEMBL201093 | 73112 | None | 0 | Human | Functional | Ki | = | 33.70 | 7.47 | - | 5 | Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay | ChEMBL | 257.1 | 0 | 0 | 2 | 3.37 | CN1CCc2ccccc2Cc2ccsc2CC1 | https://dx.doi.org/10.1021/jm050846j | |
CHEMBL201170 | 73177 | None | 0 | Human | Functional | Ki | = | 1.69 | 8.77 | - | 6 | Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay | ChEMBL | 267.2 | 0 | 1 | 2 | 3.01 | CN1CCc2ccccc2Cc2ccc(O)cc2CC1 | https://dx.doi.org/10.1021/jm050846j | |
CHEMBL201170 | 73177 | None | 0 | Human | Functional | Ki | = | 1.69 | 8.77 | - | 6 | Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay | ChEMBL | 267.2 | 0 | 1 | 2 | 3.01 | CN1CCc2ccccc2Cc2ccc(O)cc2CC1 | https://dx.doi.org/10.1021/jm051237e | |
CHEMBL201483 | 73411 | None | 0 | Human | Functional | Ki | = | 337.00 | 6.47 | - | 4 | Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay | ChEMBL | 254.2 | 0 | 0 | 2 | 2.65 | CN1CCc2ccccc2Cc2ccn(C)c2CC1 | https://dx.doi.org/10.1021/jm050846j | |
CHEMBL201525 | 73420 | None | 0 | Human | Functional | Ki | = | 3.09 | 8.51 | - | 6 | Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay | ChEMBL | 251.2 | 0 | 0 | 1 | 3.31 | CN1CCc2ccccc2Cc2ccccc2CC1 | https://dx.doi.org/10.1021/jm050846j | |
CHEMBL201584 | 73433 | None | 5 | Human | Functional | Ki | = | 112.00 | 6.95 | - | 3 | Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay | ChEMBL | 304.2 | 1 | 1 | 1 | 4.37 | CN1CCc2c([nH]c3ccccc23)CC(c2ccccc2)CC1 | https://dx.doi.org/10.1021/jm050846j | |
CHEMBL203029 | 74720 | None | 0 | Human | Functional | Ki | = | 2.32 | 8.63 | - | 4 | Inhibition of binding to human D5 receptor expressed in HEK 293 cells by functional calcium assay | ChEMBL | 283.2 | 0 | 2 | 3 | 2.72 | CN1CCc2ccccc2Cc2cc(O)c(O)cc2CC1 | https://dx.doi.org/10.1021/jm050846j | |
CHEMBL203047 | 74725 | None | 0 | Human | Functional | Ki | = | 3.10 | 8.51 | - | 4 | Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay | ChEMBL | 301.1 | 0 | 1 | 2 | 3.67 | CN1CCc2ccccc2Cc2cc(O)c(Cl)cc2CC1 | https://dx.doi.org/10.1021/jm051237e | |
CHEMBL203637 | 75199 | None | 0 | Human | Functional | Ki | = | 0.05 | 10.28 | - | 6 | Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay | ChEMBL | 301.1 | 0 | 1 | 2 | 3.67 | CN1CCc2ccccc2Cc2ccc(O)c(Cl)c2CC1 | https://dx.doi.org/10.1021/jm051237e | |
CHEMBL203689 | 75278 | None | 0 | Human | Functional | Ki | = | 10.40 | 7.98 | - | 4 | Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay | ChEMBL | 267.2 | 0 | 1 | 2 | 3.01 | CN1CCc2ccccc2Cc2c(O)cccc2CC1 | https://dx.doi.org/10.1021/jm051237e | |
CHEMBL203734 | 75317 | None | 0 | Human | Functional | Ki | = | 59.00 | 7.23 | - | 4 | Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay | ChEMBL | 349.1 | 1 | 0 | 2 | 4.62 | COc1c(Cl)cc2c(c1Cl)Cc1ccccc1CCN(C)CC2 | https://dx.doi.org/10.1021/jm051237e | |
CHEMBL204065 | 75443 | None | 0 | Human | Functional | Ki | = | 11.50 | 7.94 | - | 4 | Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay | ChEMBL | 311.2 | 2 | 0 | 3 | 3.33 | COc1ccc2c(c1)CCN(C)CCc1cc(OC)ccc1C2 | https://dx.doi.org/10.1021/jm051237e | |
CHEMBL204098 | 75449 | None | 0 | Human | Functional | Ki | = | 39.50 | 7.40 | - | 3 | Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay | ChEMBL | 282.2 | 0 | 2 | 3 | 2.60 | CN1CCc2ccccc2Cc2cc(N)c(O)cc2CC1 | https://dx.doi.org/10.1021/jm051237e | |
CHEMBL216258 | 81612 | None | 0 | Human | Functional | Ki | = | 2.80 | 8.55 | - | 5 | Activity at human D5 dopamine receptor expressed in HEK293 cells by calcium fluorescence assay | ChEMBL | 304.2 | 0 | 1 | 1 | 4.18 | CN1CCCc2ccccc2Cc2[nH]c3ccccc3c2CC1 | https://dx.doi.org/10.1021/jm060213k | |
CHEMBL216439 | 81864 | None | 0 | Human | Functional | Ki | = | 71.60 | 7.14 | - | 6 | Activity at human D5 dopamine receptor expressed in HEK293 cells by calcium fluorescence assay | ChEMBL | 304.2 | 0 | 1 | 1 | 4.18 | CN1CCCc2c([nH]c3ccccc23)Cc2ccccc2CC1 | https://dx.doi.org/10.1021/jm060213k | |
CHEMBL3697578 | 132505 | None | 15 | Human | Functional | EC50 | = | 12.00 | 7.92 | -2 | 2 | Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay | ChEMBL | 389.1 | 5 | 1 | 6 | 3.15 | Cc1cc(Oc2ncccc2OC(F)F)ccc1-c1c(C)c(=O)[nH]c(=O)n1C | https://dx.doi.org/10.1021/acsmedchemlett.9b00050 | |
CHEMBL379662 | 139642 | None | 0 | Human | Functional | Ki | = | 54.60 | 7.26 | - | 4 | Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay | ChEMBL | 281.2 | 1 | 0 | 2 | 3.32 | COc1cccc2c1Cc1ccccc1CCN(C)CC2 | https://dx.doi.org/10.1021/jm051237e | |
CHEMBL380330 | 140252 | None | 0 | Human | Functional | Ki | = | 7.20 | 8.14 | - | 6 | Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay | ChEMBL | 281.2 | 1 | 0 | 2 | 3.32 | COc1ccc2c(c1)CCN(C)CCc1ccccc1C2 | https://dx.doi.org/10.1021/jm051237e | |
CHEMBL380464 | 140275 | None | 0 | Human | Functional | Ki | = | 1.60 | 8.80 | - | 4 | Inhibition of D5 dopamine receptor in HEK 293 cells by intracellular calcium assay | ChEMBL | 301.1 | 0 | 1 | 2 | 3.67 | CN1CCc2ccccc2Cc2c(ccc(O)c2Cl)CC1 | https://dx.doi.org/10.1021/jm051237e |
Showing 1 to 20 of 34 entries