| Assay ID | Title | Year | Journal | Article |
|---|
| AID66344 | Inhibitory concentration against Endothelin A receptor | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
| Selective optimization of side activities: another way for drug discovery. |
| AID66044 | Tested for binding affinity against ETA receptor via inhibition of ET-1 induced contractions in rabbit carotid artery ring | 2002 | Bioorganic & medicinal chemistry letters, Feb-25, Volume: 12, Issue:4
| Biphenylsulfonamide endothelin receptor antagonists. Part 3: structure-activity relationship of 4'-heterocyclic biphenylsulfonamides. |
| AID37706 | Compound was evaluated for its binding affinity towards rat Angiotensin II receptor, type 1 | 2002 | Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
| Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists. |
| AID25496 | Area under curve at intravenous dose of 50 umol/kg in monkey | 2003 | Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
| Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective |
| AID29824 | Percent oral bioavailability at dose of 50 umol/kg in monkey | 2003 | Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
| Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective |
| AID250063 | Endothelin pressor effect in rats after oral dose of 30 uM/kg | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
| Dual angiotensin II and endothelin A receptor antagonists: synthesis of 2'-substituted N-3-isoxazolyl biphenylsulfonamides with improved potency and pharmacokinetics. |
| AID30146 | Tested for volume distribution at intravenous dose of 50 umol/kg in monkey | 2003 | Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
| Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective |
| AID27771 | MRT value was calculated | 2003 | Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
| Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective |
| AID29711 | T max value at oral dose of 50 umol/kg in monkey | 2003 | Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
| Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective |
| AID185058 | Compound was tested for its activity in Ang II pressor test following oral administration; NE = No effect | 2002 | Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
| Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists. |
| AID68490 | Binding affinity to CHO cells stably expressing human Endothelin A receptor. | 2002 | Bioorganic & medicinal chemistry letters, Feb-25, Volume: 12, Issue:4
| Biphenylsulfonamide endothelin receptor antagonists. Part 3: structure-activity relationship of 4'-heterocyclic biphenylsulfonamides. |
| AID68473 | Inhibition of Human Endothelin A receptor expressed in CHO Cells. | 2000 | Journal of medicinal chemistry, Aug-10, Volume: 43, Issue:16
| Biphenylsulfonamide endothelin receptor antagonists. 2. Discovery of 4'-oxazolyl biphenylsulfonamides as a new class of potent, highly selective ET(A) antagonists. |
| AID68487 | Inhibitory activity against human endothelin A receptor expressed in CHO cells | 2003 | Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
| Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective |
| AID166801 | Inhibition of Endothelin-1 induced contractions in rabbit carotid artery rings. | 2000 | Journal of medicinal chemistry, Aug-10, Volume: 43, Issue:16
| Biphenylsulfonamide endothelin receptor antagonists. 2. Discovery of 4'-oxazolyl biphenylsulfonamides as a new class of potent, highly selective ET(A) antagonists. |
| AID1626390 | Displacement of [125I]-ET1 from ETB receptor in rat cerebellum after 3 hrs by scintillation counting method | 2016 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
| From bosentan (Tracleer®) to macitentan (Opsumit®): The medicinal chemistry perspective. |
| AID66682 | Inhibition of Human Endothelin B receptor expressed in CHO Cells. | 2000 | Journal of medicinal chemistry, Aug-10, Volume: 43, Issue:16
| Biphenylsulfonamide endothelin receptor antagonists. 2. Discovery of 4'-oxazolyl biphenylsulfonamides as a new class of potent, highly selective ET(A) antagonists. |
| AID8391 | Compound was evaluated for oral bioavailability in rats | 2004 | Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8
| Discovery, modeling, and human pharmacokinetics of N-(2-acetyl-4,6-dimethylphenyl)-3-(3,4-dimethylisoxazol-5-ylsulfamoyl)thiophene-2-carboxamide (TBC3711), a second generation, ETA selective, and orally bioavailable endothelin antagonist. |
| AID707870 | Binding affinity to AT1 receptor | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Chemokine receptor antagonists. |
| AID66693 | Binding affinity to CHO cells stably expressing human Endothelin B receptor. | 2002 | Bioorganic & medicinal chemistry letters, Feb-25, Volume: 12, Issue:4
| Biphenylsulfonamide endothelin receptor antagonists. Part 3: structure-activity relationship of 4'-heterocyclic biphenylsulfonamides. |
| AID66210 | Binding affinity towards Endothelin A receptor | 2004 | Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8
| Discovery, modeling, and human pharmacokinetics of N-(2-acetyl-4,6-dimethylphenyl)-3-(3,4-dimethylisoxazol-5-ylsulfamoyl)thiophene-2-carboxamide (TBC3711), a second generation, ETA selective, and orally bioavailable endothelin antagonist. |
| AID29707 | T max value at oral dose of 10 umol/kg in rat | 2003 | Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
| Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective |
| AID66690 | Inhibitory activity against human endothelin B receptor expressed in CHO cells | 2003 | Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
| Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective |
| AID166800 | In vitro inhibition of ET-1 induced contractions in rabbit carotid artery rings | 2003 | Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
| Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective |
| AID67339 | Inhibitory concentration against endotheline ETB receptor | 2004 | Journal of medicinal chemistry, Mar-11, Volume: 47, Issue:6
| Selective optimization of side activities: another way for drug discovery. |
| AID27210 | Half life in rat | 2003 | Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
| Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective |
| AID66214 | Selectivity for endothelin A receptor over endothelin receptor B | 2004 | Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8
| Discovery, modeling, and human pharmacokinetics of N-(2-acetyl-4,6-dimethylphenyl)-3-(3,4-dimethylisoxazol-5-ylsulfamoyl)thiophene-2-carboxamide (TBC3711), a second generation, ETA selective, and orally bioavailable endothelin antagonist. |
| AID28065 | C max value at oral dose of 10 umol/kg in rat | 2003 | Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
| Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective |
| AID27205 | Half life in monkey at intravenous dose of 50 umol/kg | 2003 | Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
| Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective |
| AID178547 | Compound was tested for its activity in bET-1 pressor test following oral administration | 2002 | Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
| Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists. |
| AID12105 | Half life period was evaluated in rat | 2004 | Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8
| Discovery, modeling, and human pharmacokinetics of N-(2-acetyl-4,6-dimethylphenyl)-3-(3,4-dimethylisoxazol-5-ylsulfamoyl)thiophene-2-carboxamide (TBC3711), a second generation, ETA selective, and orally bioavailable endothelin antagonist. |
| AID68482 | Compound was evaluated for its binding affinity towards human Endothelin A receptor | 2002 | Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
| Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists. |
| AID30142 | Tested for volume distribution at intravenous dose of 10 umol/kg in rat | 2003 | Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
| Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective |
| AID27207 | Half life in monkey at oral dose of 50 umol/kg | 2003 | Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
| Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective |
| AID707869 | Binding affinity to ETA receptor | 2012 | Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
| Chemokine receptor antagonists. |
| AID12753 | Compound was evaluated for oral bioavailability in rats | 2004 | Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8
| Discovery, modeling, and human pharmacokinetics of N-(2-acetyl-4,6-dimethylphenyl)-3-(3,4-dimethylisoxazol-5-ylsulfamoyl)thiophene-2-carboxamide (TBC3711), a second generation, ETA selective, and orally bioavailable endothelin antagonist. |
| AID27888 | Tested for plasma clearance at intravenous dose of 10 umol/kg in rat | 2003 | Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
| Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective |
| AID229936 | Selectivity ratio between ET A and ET B receptors. | 2002 | Bioorganic & medicinal chemistry letters, Feb-25, Volume: 12, Issue:4
| Biphenylsulfonamide endothelin receptor antagonists. Part 3: structure-activity relationship of 4'-heterocyclic biphenylsulfonamides. |
| AID27891 | Tested for plasma clearance at intravenous dose of 50 umol/kg in monkey | 2003 | Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
| Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective |
| AID29819 | Percent oral bioavailability at dose of 10 umol/kg in rat | 2003 | Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
| Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective |
| AID28068 | C max value at oral dose of 50 umol/kg in monkey | 2003 | Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
| Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective |
| AID39788 | Compound was evaluated for its binding affinity towards human Angiotensin II receptor, type 1 | 2002 | Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
| Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists. |
| AID8393 | Half life period was evaluated in monkey | 2004 | Journal of medicinal chemistry, Apr-08, Volume: 47, Issue:8
| Discovery, modeling, and human pharmacokinetics of N-(2-acetyl-4,6-dimethylphenyl)-3-(3,4-dimethylisoxazol-5-ylsulfamoyl)thiophene-2-carboxamide (TBC3711), a second generation, ETA selective, and orally bioavailable endothelin antagonist. |
| AID1626384 | Displacement of [125I]-ET1 from ETA receptor in A10 rat thoracic aorta smooth muscle after 3 hrs by scintillation counting method | 2016 | Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
| From bosentan (Tracleer®) to macitentan (Opsumit®): The medicinal chemistry perspective. |
| AID26959 | cLogP value of the compound | 2003 | Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
| Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective |
| AID249997 | Permeability in Caco-2 cell monolayer | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
| Dual angiotensin II and endothelin A receptor antagonists: synthesis of 2'-substituted N-3-isoxazolyl biphenylsulfonamides with improved potency and pharmacokinetics. |
| AID184926 | Compound was tested for its activity in Ang II pressor test following intravenous administration; NE = No effect | 2002 | Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
| Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists. |
| AID28400 | Permeability (caco-2 cell assay) | 2003 | Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
| Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective |
| AID25498 | Area under curve at oral dose of 50 umol/kg in monkey | 2003 | Journal of medicinal chemistry, Jan-02, Volume: 46, Issue:1
| Biphenylsulfonamide endothelin receptor antagonists. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective |
| AID250249 | Angiotensin II pressor effect in rats after oral dose of 30 uM/kg | 2005 | Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1
| Dual angiotensin II and endothelin A receptor antagonists: synthesis of 2'-substituted N-3-isoxazolyl biphenylsulfonamides with improved potency and pharmacokinetics. |
| AID178546 | Compound was tested for its activity in bET-1 pressor test following intravenous administration | 2002 | Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
| Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |