| Assay ID | Title | Year | Journal | Article |
|---|
| AID1229769 | Displacement of [3H]raclopride from wild type human dopamine D2L receptor expressed in FlpIn CHO cell membrane assessed as equilibrium dissociation constant after 3 hrs by MicroBeta counting analysis | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Structure-activity study of N-((trans)-4-(2-(7-cyano-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)cyclohexyl)-1H-indole-2-carboxamide (SB269652), a bitopic ligand that acts as a negative allosteric modulator of the dopamine D2 receptor. |
| AID1484191 | Agonist activity at D3 receptor (unknown origin) expressed in CHOK1 cells assessed as beta-arrestin recruitment up to 30 uM after 90 mins by DiscoveRx PathHunter assay | | | |
| AID1484185 | Antagonist activity at D2 long receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of dopamine induced beta-arrestin recruitment after 90 mins by DiscoveRx PathHunter assay | | | |
| AID1484192 | Allosteric antagonist activity at D3 receptor (unknown origin) expressed in CHOK1 cells assessed as fold reduction in dopamine induced beta-arrestin recruitment after 90 mins by DiscoveRx PathHunter assay | | | |
| AID1484186 | Allosteric antagonist activity at D3 receptor (unknown origin) expressed in CHOK1 cells assessed as inhibition of dopamine induced beta-arrestin recruitment after 90 mins by DiscoveRx PathHunter assay | | | |
| AID1484182 | Displacement of [3H]N-methylspiperone from human D2L receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis | | | |
| AID1513122 | Negative allosteric modulation of D2R (unknown origin) assessed as decrease in dopamine-induced response relative to control | 2019 | Journal of medicinal chemistry, 01-10, Volume: 62, Issue:1
| Subtle Modifications to the Indole-2-carboxamide Motif of the Negative Allosteric Modulator N-(( trans)-4-(2-(7-Cyano-3,4-dihydroisoquinolin-2(1 H)-yl)ethyl)cyclohexyl)-1 H-indole-2-carboxamide (SB269652) Yield Dramatic Changes in Pharmacological Activity |
| AID1513124 | Negative allosteric modulation of human D2LR expressed in Flp-In-CHO cells assessed as inhibition of dopamine-indued ERK1/2 phosphorylation preincubated for 30 mins followed by dopamine addition and measured after 5 mins by AlphaScreen assay | 2019 | Journal of medicinal chemistry, 01-10, Volume: 62, Issue:1
| Subtle Modifications to the Indole-2-carboxamide Motif of the Negative Allosteric Modulator N-(( trans)-4-(2-(7-Cyano-3,4-dihydroisoquinolin-2(1 H)-yl)ethyl)cyclohexyl)-1 H-indole-2-carboxamide (SB269652) Yield Dramatic Changes in Pharmacological Activity |
| AID1484194 | Non-competitive antagonist activity at D3 receptor (unknown origin) expressed in CHOK1 cells assessed as induction of rightward shift in the dopamine dose response curve for beta-arrestin recruitment after 90 mins by DiscoveRx PathHunter assay | | | |
| AID1513125 | Negative allosteric modulation of human D2LR expressed in Flp-In-CHO cells assessed as inhibition of dopamine-indued ERK1/2 phosphorylation by measuring negative co-operativity factor preincubated for 30 mins followed by dopamine addition and measured aft | 2019 | Journal of medicinal chemistry, 01-10, Volume: 62, Issue:1
| Subtle Modifications to the Indole-2-carboxamide Motif of the Negative Allosteric Modulator N-(( trans)-4-(2-(7-Cyano-3,4-dihydroisoquinolin-2(1 H)-yl)ethyl)cyclohexyl)-1 H-indole-2-carboxamide (SB269652) Yield Dramatic Changes in Pharmacological Activity |
| AID1513123 | Negative allosteric modulation of D2R (unknown origin) | 2019 | Journal of medicinal chemistry, 01-10, Volume: 62, Issue:1
| Subtle Modifications to the Indole-2-carboxamide Motif of the Negative Allosteric Modulator N-(( trans)-4-(2-(7-Cyano-3,4-dihydroisoquinolin-2(1 H)-yl)ethyl)cyclohexyl)-1 H-indole-2-carboxamide (SB269652) Yield Dramatic Changes in Pharmacological Activity |
| AID1484183 | Displacement of [3H]N-methylspiperone from human D3 receptor expressed in HEK293 cell membranes after 1 hr by liquid scintillation counting analysis | | | |
| AID1513126 | Negative allosteric modulation of human D2LR expressed in Flp-In-CHO cells assessed as inhibition of dopamine-indued ERK1/2 phosphorylation preincubated for 30 mins followed by dopamine addition and measured after 5 mins by AlphaScreen assay relative to c | 2019 | Journal of medicinal chemistry, 01-10, Volume: 62, Issue:1
| Subtle Modifications to the Indole-2-carboxamide Motif of the Negative Allosteric Modulator N-(( trans)-4-(2-(7-Cyano-3,4-dihydroisoquinolin-2(1 H)-yl)ethyl)cyclohexyl)-1 H-indole-2-carboxamide (SB269652) Yield Dramatic Changes in Pharmacological Activity |
| AID1229770 | Negative allosteric modulator activity at wild type human dopamine D2L receptor expressed in FlpIn CHO cell membrane assessed as ERK1/2 phosphorylation measured as equilibrium dissociation constant after 30 mins | 2015 | Journal of medicinal chemistry, Jul-09, Volume: 58, Issue:13
| Structure-activity study of N-((trans)-4-(2-(7-cyano-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)cyclohexyl)-1H-indole-2-carboxamide (SB269652), a bitopic ligand that acts as a negative allosteric modulator of the dopamine D2 receptor. |
| AID1484190 | Agonist activity at D2 long receptor (unknown origin) expressed in CHOK1 cells assessed as beta-arrestin recruitment up to 30 uM after 90 mins by DiscoveRx PathHunter assay | | | |
| AID1513121 | Negative allosteric modulation of D2R (unknown origin) assessed as negative co-operativity factor | 2019 | Journal of medicinal chemistry, 01-10, Volume: 62, Issue:1
| Subtle Modifications to the Indole-2-carboxamide Motif of the Negative Allosteric Modulator N-(( trans)-4-(2-(7-Cyano-3,4-dihydroisoquinolin-2(1 H)-yl)ethyl)cyclohexyl)-1 H-indole-2-carboxamide (SB269652) Yield Dramatic Changes in Pharmacological Activity |
| AID1484184 | Selectivity ratio of Ki for human D2 receptor to Ki for human D3 receptor | | | |
| AID1345788 | Human D2 receptor (Dopamine receptors) | 2014 | Nature chemical biology, Sep, Volume: 10, Issue:9
| A new mechanism of allostery in a G protein-coupled receptor dimer. |
| AID1345833 | Human D3 receptor (Dopamine receptors) | 2015 | European neuropsychopharmacology : the journal of the European College of Neuropsychopharmacology, Sep, Volume: 25, Issue:9
| Investigation of the binding and functional properties of extended length D3 dopamine receptor-selective antagonists. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |