Assay ID | Title | Year | Journal | Article |
AID3865 | Ability to displace [3H]5-CT (2.0 nM) from HeLa cells of human 5-hydroxytryptamine 1A receptor; NT denotes not tested | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
| Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists. |
AID5475 | Ability to displace [3H]ketanserin (0.5 nM) from cerebral cortex of rat 5-hydroxytryptamine 2A receptor | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
| Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists. |
AID61018 | Ability to inhibit binding of [3H]-SCH- 23390 to Dopamine receptor D1 in rat striatal membranes | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
| Octoclothepin enantiomers. A reinvestigation of their biochemical and pharmacological activity in relation to a new receptor-interaction model for dopamine D-2 receptor antagonists. |
AID65296 | Ability to displace [3H]spiperone (0.3 nM) from CHO cells of human Dopamine receptor D3; NT denotes not tested | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
| Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists. |
AID225276 | Dose to antagonise, when given subcutaneously to 6-OH-DA-lesioned rats, using pergolide antagonism test.(in vivo) | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
| Octoclothepin enantiomers. A reinvestigation of their biochemical and pharmacological activity in relation to a new receptor-interaction model for dopamine D-2 receptor antagonists. |
AID5058 | Ability to inhibit binding of [3H]KET to 5-hydroxytryptamine 2 receptor in rat cortex | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
| Octoclothepin enantiomers. A reinvestigation of their biochemical and pharmacological activity in relation to a new receptor-interaction model for dopamine D-2 receptor antagonists. |
AID61543 | Binding affinity towardst dopamine D2 receptor by displacement of [3H]-SPI radioligand in rat striatal membranes | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
| A structure-activity study of four dopamine D-1 and D-2 receptor antagonists, representing the phenylindan, -indene, and -indole structural classes of compounds. |
AID225278 | Dose to antagonise, when given subcutaneously to rats (in vivo) using flexor reflex St 587 antagonism test. | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
| Octoclothepin enantiomers. A reinvestigation of their biochemical and pharmacological activity in relation to a new receptor-interaction model for dopamine D-2 receptor antagonists. |
AID5326 | Half-maximal inhibition of [3H]- Ketanserin binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex homogenate | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
| Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies. |
AID179756 | In vitro inhibition of the accumulation of [3H]-NE into rat brain synaptosomes | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
| Octoclothepin enantiomers. A reinvestigation of their biochemical and pharmacological activity in relation to a new receptor-interaction model for dopamine D-2 receptor antagonists. |
AID61383 | Ability to displace [3H]spiperone (0.5 nM) from corpus striatum of rat Dopamine receptor D2 | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
| Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists. |
AID65619 | Half-maximal inhibition of [3H]-7-OH-DPAT binding to Dopamine receptor D3 in rat tissue homogenate | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
| Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies. |
AID225277 | Dose to antagonise, when given subcutaneously to rats (in vivo) using catalepsy test, maximum effect 1-6h. | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
| Octoclothepin enantiomers. A reinvestigation of their biochemical and pharmacological activity in relation to a new receptor-interaction model for dopamine D-2 receptor antagonists. |
AID65622 | In vitro binding affinity towards Dopamine receptor D3 in Sf9 cell membranes using [3H]7-OH-DPAT as radioligand | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
| Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents. |
AID63809 | Half-maximal inhibition of [3H]spiperone binding to Dopamine receptor D2 in rat striatal homogenate | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
| Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies. |
AID229410 | Selectivity ratio (5-HT2A/D2 ) | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
| Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies. |
AID61034 | Binding affinity towards dopamine receptor D1 by displacement of [3H]-SCH- radioligand in rat striatal membranes | 1993 | Journal of medicinal chemistry, Oct-01, Volume: 36, Issue:20
| A structure-activity study of four dopamine D-1 and D-2 receptor antagonists, representing the phenylindan, -indene, and -indole structural classes of compounds. |
AID517788 | Displacement of [3H]prozosin from bovine cloned Alpha-1A receptor expressed in BHK cells | 2010 | Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
| Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity for α(1)-adrenoceptors. |
AID61545 | Binding affinity at dopamine D2 receptor by [3H]spiperone displacement. | 1994 | Journal of medicinal chemistry, Apr-01, Volume: 37, Issue:7
| Development of a receptor-interaction model for serotonin 5-HT2 receptor antagonists. Predicting selectivity with respect to dopamine D2 receptors. |
AID225275 | Dose to antagonise, when given subcutaneously to 6-OH-DA-lesioned rats, using SK & F 38393 antagonism test.(in vivo) | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
| Octoclothepin enantiomers. A reinvestigation of their biochemical and pharmacological activity in relation to a new receptor-interaction model for dopamine D-2 receptor antagonists. |
AID179754 | In vitro inhibition of the accumulation of [3H]5-HT into rat brain synaptosomes | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
| Octoclothepin enantiomers. A reinvestigation of their biochemical and pharmacological activity in relation to a new receptor-interaction model for dopamine D-2 receptor antagonists. |
AID36455 | Displacement of [3H]prazosin (0.3 nM) from bovine Alpha-1A adrenergic receptor expressed in BHK cells | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
| Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists. |
AID61675 | Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
| Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies. |
AID65948 | Displacement of [3H]-YM-09151-2 (0.06 nM) from human Dopamine receptor D4 expressed in CHO cells | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
| Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists. |
AID225279 | Dose to antagonise, when given subcutaneously to rats (in vivo) using inhibition of locomotor motility test | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
| Octoclothepin enantiomers. A reinvestigation of their biochemical and pharmacological activity in relation to a new receptor-interaction model for dopamine D-2 receptor antagonists. |
AID4791 | Binding affinity at serotonin 5-hydroxytryptamine 2 receptor by [3H]ketanserin displacement. | 1994 | Journal of medicinal chemistry, Apr-01, Volume: 37, Issue:7
| Development of a receptor-interaction model for serotonin 5-HT2 receptor antagonists. Predicting selectivity with respect to dopamine D2 receptors. |
AID61386 | Ability to inhibit binding of [3H]-SPI to dopamine receptor D2 in rat striatal membranes | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
| Octoclothepin enantiomers. A reinvestigation of their biochemical and pharmacological activity in relation to a new receptor-interaction model for dopamine D-2 receptor antagonists. |
AID36594 | Ability to inhibit binding of [3H]PRAZ to alpha-1 adrenergic receptor in rat brain | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
| Octoclothepin enantiomers. A reinvestigation of their biochemical and pharmacological activity in relation to a new receptor-interaction model for dopamine D-2 receptor antagonists. |
AID61527 | In vitro binding affinity towards Dopamine receptor D1 in rat tissue homogenate using [3H]-SCH- 23390 as radioligand | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
| Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents. |
AID517793 | Displacement of [3H]prozosin from human cloned histamine H1 receptor expressed in CHO cells | 2010 | Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
| Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity for α(1)-adrenoceptors. |
AID5569 | In vitro binding affinity towards 5-hydroxytryptamine 2A receptor in rat tissue homogenate using [3H]ketanserin as radioligand | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
| Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents. |
AID5748 | Ability to displace [3H]mesulergine (0.5 nM) from SR-3T3 cells of rat 5-hydroxytryptamine 2C receptor; NT denotes not tested | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
| Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists. |
AID4265 | Ability to displace [3H]-5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor; NT denotes not tested | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
| Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists. |
AID229417 | Selectivity ratio (D3/D1) | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
| Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies. |
AID24452 | logY value was determined | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
| Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents. |
AID225280 | Dose to antagonise, when given subcutaneously to rats (in vivo) using quipazine antagonism test. | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
| Octoclothepin enantiomers. A reinvestigation of their biochemical and pharmacological activity in relation to a new receptor-interaction model for dopamine D-2 receptor antagonists. |
AID517790 | Displacement of [3H]prozosin from rat cloned alpha1d receptor | 2010 | Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
| Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity for α(1)-adrenoceptors. |
AID179755 | In vitro inhibition of the accumulation of [3H]DA into rat brain synaptosomes | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
| Octoclothepin enantiomers. A reinvestigation of their biochemical and pharmacological activity in relation to a new receptor-interaction model for dopamine D-2 receptor antagonists. |
AID36591 | Ability to displace [3H]prazosin (0.25 nM) from whole brain of rat Alpha-1 adrenergic receptor | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
| Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists. |
AID232153 | Ratio of 5-HT2A receptor to that of dopamine 2 (D2) receptor in rat tissue homogenate | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
| Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents. |
AID517792 | Displacement of [3H]prozosin from human cloned dopamine D2 receptor expressed in CHO cells | 2010 | Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
| Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity for α(1)-adrenoceptors. |
AID223292 | Dose to antagonise, when given subcutaneously to mice (in vivo) using methyl phenidate antagonism test | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
| Octoclothepin enantiomers. A reinvestigation of their biochemical and pharmacological activity in relation to a new receptor-interaction model for dopamine D-2 receptor antagonists. |
AID517791 | Displacement of [3H]prozosin from human cloned 5HT2C receptor expressed in CHO cells | 2010 | Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
| Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity for α(1)-adrenoceptors. |
AID35591 | Displacement of [3H]prazosin (0.3 nM) from rat Alpha-1D adrenergic receptor expressed in CHO cells | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
| Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists. |
AID229416 | Selectivity ratio (D1/D2) | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
| Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies. |
AID61546 | Binding affinity against Dopamine receptor D2 using [3H]spiroperidol | 1988 | Journal of medicinal chemistry, Feb, Volume: 31, Issue:2
| Conformational analysis and structural comparisons of (1R,3S)-(+)- and (1S,3R)-(-)-tefludazine, (S)-(+)- and (R)-(-)-octoclothepin, and (+)-dexclamol in relation to dopamine receptor antagonism and amine-uptake inhibition. |
AID517789 | Displacement of [3H]prozosin from hamster cloned alpha-1b receptor | 2010 | Journal of medicinal chemistry, Oct-14, Volume: 53, Issue:19
| Exploring the neuroleptic substituent in octoclothepin: potential ligands for positron emission tomography with subnanomolar affinity for α(1)-adrenoceptors. |
AID5560 | Half-maximal inhibition of [3H]ketanserin binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex homogenate | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
| Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies. |
AID65733 | In vitro binding affinity towards Dopamine receptor D2 in rat tissue homogenate using [3H]-spiperone as radioligand | 2004 | Journal of medicinal chemistry, Jan-01, Volume: 47, Issue:1
| Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents. |
AID65563 | Half-maximal inhibition of [3H]spiperone binding to Dopamine receptor D2 in rat striatal homogenate | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
| Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies. |
AID61016 | Ability to displace [3H]-SCH- 23390 (0.2 nM) from corpus striatum of rat Dopamine receptor D1 | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
| Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists. |
AID61517 | Half-maximal inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 in rat striatal homogenate | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
| Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies. |
AID37067 | Displacement of [3H]prazosin (0.5 nM) from hamster Alpha-1B adrenergic receptor expressed in rat-1 cells | 2003 | Journal of medicinal chemistry, Jan-16, Volume: 46, Issue:2
| Synthesis and structure-affinity relationship investigations of 5-heteroaryl-substituted analogues of the antipsychotic sertindole. A new class of highly selective alpha(1) adrenoceptor antagonists. |
AID65767 | Half-maximal inhibition of [3H]7-OH-DPAT binding to Dopamine receptor D3 in rat tissue homogenate | 2002 | Journal of medicinal chemistry, Jan-17, Volume: 45, Issue:2
| Pyrrolo[1,3]benzothiazepine-based atypical antipsychotic agents. Synthesis, structure-activity relationship, molecular modeling, and biological studies. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |