Relation Results

Summary

Name ADRA1D
Full Name Alpha-1D adrenergic receptor
Synonyms Alpha-1A adrenergic receptor, Alpha-1D adrenoreceptor, Alpha-1D adrenoceptor, Alpha-adrenergic receptor 1a | ADRA1A
Primary ID P25100
Links - -
Type protein
Relations 18
Inhibitors prazosin; 8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-8-azaspiro[4.5]decane-7,9-dione; silodosin; terazosin; phentolamine; N-(2,3-dihydro-1,4-benzodioxin-2-ylmethyl)-2-(2,6-dimethoxyphenoxy)ethanamine; tamsulosin; (4S)-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid O5-[3-(4,4-diphenyl-1-piperidinyl)propyl] ester O3-methyl ester
Function This alpha-adrenergic receptor mediates its effect through the influx of extracellular calcium.

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Type: Score: Layout: SPV 
0.80.80.80.80.2780.80.80.80.2910.80.80.80.5830.80.80.4340.8(R)-adrenalineADRA1Dprazosin8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-8-azaspiro[4.5]decane-7,9-dionesilodosinGNALmethoxamineoxymetazoline(R)-noradrenalineGNAS(S)-adrenalineterazosinphentolamineGNAQN-(2,3-dihydro-1,4-benzodioxin-2-ylmethyl)-2-(2,6-dimethoxyphenoxy)ethanaminetamsulosinGNA14(4S)-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid O5-[3-(4,4-diphenyl-1-piperidinyl)propyl] ester O3-methyl ester

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Relations
Regulator
Mechanism
target
score ℹ
+ (R)-adrenalineup-regulates activity img/direct-activation.png chemical activation ADRA1D 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258459 Cricetulus griseus CHO Cell
pmid sentence
Membrane preparations from CHO cells stably transfected with the cloned human a1-AR genes showed saturable binding of [‘251]HEAT; Bm,,ı values were 1.3 ± 0.2, 5.5 ± 0.1, and 1.1 ± 0.1 pmol/mg of protein, with Kd values of 110 ± 21, 60 ± 1, and 300 ± 26 ıM (three experiments each), for the ala-, alb-, and ald-ARS, respectively. The potencies of a1-AR agonists and antagonists at the cloned human a1-ARs are shown in Table 1.
Publications: 1 Organism: Cricetulus Griseus
+ prazosindown-regulates activity img/direct_inhibition.png chemical inhibition ADRA1D 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258468 Cricetulus griseus CHO Cell
pmid sentence
Membrane preparations from CHO cells stably transfected with the cloned human a1-AR genes showed saturable binding of [‘251]HEAT; Bm,,ı values were 1.3 ± 0.2, 5.5 ± 0.1, and 1.1 ± 0.1 pmol/mg of protein, with Kd values of 110 ± 21, 60 ± 1, and 300 ± 26 ıM (three experiments each), for the ala-, alb-, and ald-ARS, respectively. The potencies of a1-AR agonists and antagonists at the cloned human a1-ARs are shown in Table 1.
Publications: 1 Organism: Cricetulus Griseus
+ 8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-8-azaspiro[4.5]decane-7,9-dionedown-regulates img/direct_inhibition.png chemical inhibition ADRA1D 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-190642 Homo sapiens
pmid sentence
Publications: 1 Organism: Homo Sapiens
+ silodosindown-regulates activity img/direct_inhibition.png chemical inhibition ADRA1D 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258451 Cricetulus griseus
pmid sentence
Membrane preparations from CHO cells stably transfected with the cloned human a1-AR genes showed saturable binding of [‘251]HEAT; Bm,,ı values were 1.3 ± 0.2, 5.5 ± 0.1, and 1.1 ± 0.1 pmol/mg of protein, with Kd values of 110 ± 21, 60 ± 1, and 300 ± 26 ıM (three experiments each), for the ala-, alb-, and ald-ARS, respectively. The potencies of a1-AR agonists and antagonists at the cloned human a1-ARs are shown in Table 1.
Publications: 1 Organism: Cricetulus Griseus
+ ADRA1Dup-regulates activity img/direct-activation.png binding GNAL 0.278
Identifier Residue Sequence Organism Cell Line
SIGNOR-256951 Homo sapiens HEK-293A Cell
pmid sentence
Here we systematically quantified ligand-induced interactions between 148 GPCRs and all 11 unique G alpha subunit C-termini. For each receptor, we probed chimeric G alpha subunit activation via a transforming growth factor-alpha (TGF alpha) shedding response in HEK293 cells lacking endogenous Gq/11- and G12/13- signaling. | We defined positive coupling if any member of the subfamily scored LogRAi ≥ -1 and negative coupling if all of the members scored LogRAi < -1 (Figure 3A-B). ROC analysis gives AUC = 0.78 (Figure S4A) when considering high-confidence known coupling data and suggested a threshold of LogRAi ≥ -1.0 for defining true couplings. | The score associated to this interaction has a LogRAi ≥ -1.0.
Publications: 1 Organism: Homo Sapiens
+ methoxamineup-regulates activity img/direct-activation.png chemical activation ADRA1D 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258448 Cricetulus griseus CHO Cell
pmid sentence
Membrane preparations from CHO cells stably transfected with the cloned human a1-AR genes showed saturable binding of [‘251]HEAT; Bm,,ı values were 1.3 ± 0.2, 5.5 ± 0.1, and 1.1 ± 0.1 pmol/mg of protein, with Kd values of 110 ± 21, 60 ± 1, and 300 ± 26 ıM (three experiments each), for the ala-, alb-, and ald-ARS, respectively. The potencies of a1-AR agonists and antagonists at the cloned human a1-ARs are shown in Table 1.
Publications: 1 Organism: Cricetulus Griseus
+ oxymetazolineup-regulates activity img/direct-activation.png chemical activation ADRA1D 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258460 Cricetulus griseus CHO Cell
pmid sentence
Membrane preparations from CHO cells stably transfected with the cloned human a1-AR genes showed saturable binding of [‘251]HEAT; Bm,,ı values were 1.3 ± 0.2, 5.5 ± 0.1, and 1.1 ± 0.1 pmol/mg of protein, with Kd values of 110 ± 21, 60 ± 1, and 300 ± 26 ıM (three experiments each), for the ala-, alb-, and ald-ARS, respectively. The potencies of a1-AR agonists and antagonists at the cloned human a1-ARs are shown in Table 1.
Publications: 1 Organism: Cricetulus Griseus
+ (R)-noradrenalineup-regulates activity img/direct-activation.png chemical activation ADRA1D 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258457 Cricetulus griseus CHO Cell
pmid sentence
Membrane preparations from CHO cells stably transfected with the cloned human a1-AR genes showed saturable binding of [‘251]HEAT; Bm,,ı values were 1.3 ± 0.2, 5.5 ± 0.1, and 1.1 ± 0.1 pmol/mg of protein, with Kd values of 110 ± 21, 60 ± 1, and 300 ± 26 ıM (three experiments each), for the ala-, alb-, and ald-ARS, respectively. The potencies of a1-AR agonists and antagonists at the cloned human a1-ARs are shown in Table 1.
Identifier Residue Sequence Organism Cell Line
SIGNOR-257452 Homo sapiens HEK-293A Cell
pmid sentence
Here we systematically quantified ligand-induced interactions between 148 GPCRs and all 11 unique G alpha subunit C-termini. For each receptor, we probed chimeric G alpha subunit activation via a transforming growth factor-alpha (TGF alpha) shedding response in HEK293 cells lacking endogenous Gq/11- and G12/13- signaling. | We defined positive coupling if any member of the subfamily scored LogRAi ≥ -1 and negative coupling if all of the members scored LogRAi < -1 (Figure 3A-B). ROC analysis gives AUC = 0.78 (Figure S4A) when considering high-confidence known coupling data and suggested a threshold of LogRAi ≥ -1.0 for defining true couplings. | The score associated to this interaction has a LogRAi ≥ -1.0.
Publications: 2 Organism: Cricetulus Griseus, Homo Sapiens
+ ADRA1Dup-regulates activity img/direct-activation.png binding GNAS 0.291
Identifier Residue Sequence Organism Cell Line
SIGNOR-256808 Homo sapiens
pmid sentence
Here we systematically quantified ligand-induced interactions between 148 GPCRs and all 11 unique G alpha subunit C-termini. For each receptor, we probed chimeric G alpha subunit activation via a transforming growth factor-alpha (TGF alpha) shedding response in HEK293 cells lacking endogenous Gq/11- and G12/13- signaling. | We defined positive coupling if any member of the subfamily scored LogRAi ‚â• -1 and negative coupling if all of the members scored LogRAi < -1 (Figure 3A-B). ROC analysis gives AUC = 0.78 (Figure S4A) when considering high-confidence known coupling data and suggested a threshold of LogRAi ‚â• -1.0 for defining true couplings. | The score associated to this interaction has a LogRAi ‚â• -1.0.
Publications: 1 Organism: Homo Sapiens
+ (S)-adrenalineup-regulates activity img/direct-activation.png chemical activation ADRA1D 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258452 Cricetulus griseus CHO Cell
pmid sentence
Membrane preparations from CHO cells stably transfected with the cloned human a1-AR genes showed saturable binding of [‘251]HEAT; Bm,,ı values were 1.3 ± 0.2, 5.5 ± 0.1, and 1.1 ± 0.1 pmol/mg of protein, with Kd values of 110 ± 21, 60 ± 1, and 300 ± 26 ıM (three experiments each), for the ala-, alb-, and ald-ARS, respectively. The potencies of a1-AR agonists and antagonists at the cloned human a1-ARs are shown in Table 1.
Publications: 1 Organism: Cricetulus Griseus
+ terazosindown-regulates activity img/direct_inhibition.png chemical inhibition ADRA1D 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258670 Homo sapiens
pmid sentence
Pharmacological management of benign prostatic hyperplasia (BPH) has most successfully been achieved by administration of α1 antagonists, which function via relaxation of prostatic smooth muscle. Terazosin2 (2), doxazosin3 (3), and alfuzosin4 (4), agents currently approved for this indication
Publications: 1 Organism: Homo Sapiens
+ phentolaminedown-regulates activity img/direct_inhibition.png chemical inhibition ADRA1D 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258444 Cricetulus griseus CHO Cell
pmid sentence
Membrane preparations from CHO cells stably transfected with the cloned human a1-AR genes showed saturable binding of [‘251]HEAT; Bm,,ı values were 1.3 ± 0.2, 5.5 ± 0.1, and 1.1 ± 0.1 pmol/mg of protein, with Kd values of 110 ± 21, 60 ± 1, and 300 ± 26 ıM (three experiments each), for the ala-, alb-, and ald-ARS, respectively. The potencies of a1-AR agonists and antagonists at the cloned human a1-ARs are shown in Table 1.
Publications: 1 Organism: Cricetulus Griseus
+ ADRA1Dup-regulates activity img/direct-activation.png binding GNAQ 0.583
Identifier Residue Sequence Organism Cell Line
SIGNOR-257080 Homo sapiens HEK-293A Cell
pmid sentence
Here we systematically quantified ligand-induced interactions between 148 GPCRs and all 11 unique G alpha subunit C-termini. For each receptor, we probed chimeric G alpha subunit activation via a transforming growth factor-alpha (TGF alpha) shedding response in HEK293 cells lacking endogenous Gq/11- and G12/13- signaling. | We defined positive coupling if any member of the subfamily scored LogRAi ≥ -1 and negative coupling if all of the members scored LogRAi < -1 (Figure 3A-B). ROC analysis gives AUC = 0.78 (Figure S4A) when considering high-confidence known coupling data and suggested a threshold of LogRAi ≥ -1.0 for defining true couplings. | The score associated to this interaction has a LogRAi ≥ -1.0.
Publications: 1 Organism: Homo Sapiens
+ N-(2,3-dihydro-1,4-benzodioxin-2-ylmethyl)-2-(2,6-dimethoxyphenoxy)ethanaminedown-regulates activity img/direct_inhibition.png chemical inhibition ADRA1D 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258467 Cricetulus griseus CHO Cell
pmid sentence
Membrane preparations from CHO cells stably transfected with the cloned human a1-AR genes showed saturable binding of [‘251]HEAT; Bm,,ı values were 1.3 ± 0.2, 5.5 ± 0.1, and 1.1 ± 0.1 pmol/mg of protein, with Kd values of 110 ± 21, 60 ± 1, and 300 ± 26 ıM (three experiments each), for the ala-, alb-, and ald-ARS, respectively. The potencies of a1-AR agonists and antagonists at the cloned human a1-ARs are shown in Table 1.
Publications: 1 Organism: Cricetulus Griseus
+ tamsulosindown-regulates activity img/direct_inhibition.png chemical inhibition ADRA1D 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258471 Cricetulus griseus CHO Cell
pmid sentence
Membrane preparations from CHO cells stably transfected with the cloned human a1-AR genes showed saturable binding of [‘251]HEAT; Bm,,ı values were 1.3 ± 0.2, 5.5 ± 0.1, and 1.1 ± 0.1 pmol/mg of protein, with Kd values of 110 ± 21, 60 ± 1, and 300 ± 26 ıM (three experiments each), for the ala-, alb-, and ald-ARS, respectively. The potencies of a1-AR agonists and antagonists at the cloned human a1-ARs are shown in Table 1.
Publications: 1 Organism: Cricetulus Griseus
+ ADRA1Dup-regulates activity img/direct-activation.png binding GNA14 0.434
Identifier Residue Sequence Organism Cell Line
SIGNOR-257191 Homo sapiens
pmid sentence
Here we systematically quantified ligand-induced interactions between 148 GPCRs and all 11 unique G alpha subunit C-termini. For each receptor, we probed chimeric G alpha subunit activation via a transforming growth factor-alpha (TGF alpha) shedding response in HEK293 cells lacking endogenous Gq/11- and G12/13- signaling. | We defined positive coupling if any member of the subfamily scored LogRAi ≥ -1 and negative coupling if all of the members scored LogRAi < -1 (Figure 3A-B). ROC analysis gives AUC = 0.78 (Figure S4A) when considering high-confidence known coupling data and suggested a threshold of LogRAi ≥ -1.0 for defining true couplings. | The score associated to this interaction has a LogRAi ≥ -1.0.
Publications: 1 Organism: Homo Sapiens
+ (4S)-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid O5-[3-(4,4-diphenyl-1-piperidinyl)propyl] ester O3-methyl esterdown-regulates activity img/direct_inhibition.png chemical inhibition ADRA1D 0.8
Identifier Residue Sequence Organism Cell Line
SIGNOR-258464 Cricetulus griseus CHO Cell
pmid sentence
Membrane preparations from CHO cells stably transfected with the cloned human a1-AR genes showed saturable binding of [‘251]HEAT; Bm,,ı values were 1.3 ± 0.2, 5.5 ± 0.1, and 1.1 ± 0.1 pmol/mg of protein, with Kd values of 110 ± 21, 60 ± 1, and 300 ± 26 ıM (three experiments each), for the ala-, alb-, and ald-ARS, respectively. The potencies of a1-AR agonists and antagonists at the cloned human a1-ARs are shown in Table 1.
Publications: 1 Organism: Cricetulus Griseus
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