| Assay ID | Title | Year | Journal | Article |
|---|
| AID15842 | Aqueous solubility in pH 7.4 phosphate buffer | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
| Butenolide endothelin antagonists with improved aqueous solubility. |
| AID574640 | Biodistribution on BALB/c mouse bile at 2.5 nmol/kg, iv after 30 mins in presence of PD156707 | 2011 | Journal of medicinal chemistry, Feb-24, Volume: 54, Issue:4
| Development and evaluation of endothelin-A receptor (radio)ligands for positron emission tomography. |
| AID14097 | Maximum observed concentration in oral (5 mg/kg) fed dogs | 1997 | Journal of medicinal chemistry, Mar-28, Volume: 40, Issue:7
| Structure-activity relationships in a series of orally active gamma-hydroxy butenolide endothelin antagonists. |
| AID66034 | Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells | 1997 | Journal of medicinal chemistry, Mar-28, Volume: 40, Issue:7
| Structure-activity relationships in a series of orally active gamma-hydroxy butenolide endothelin antagonists. |
| AID234515 | Selectivity of compound on ET B with respect to ET A receptor | 1997 | Journal of medicinal chemistry, Mar-28, Volume: 40, Issue:7
| Structure-activity relationships in a series of orally active gamma-hydroxy butenolide endothelin antagonists. |
| AID66520 | Inhibition of [125I]ET1 binding to recombinant human Endothelin B receptor. | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
| Butenolide endothelin antagonists with improved aqueous solubility. |
| AID452800 | Displacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomes | 2009 | Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20
| PET-compatible endothelin receptor radioligands: synthesis and first in vitro and in vivo studies. |
| AID68315 | Inhibition of [125I]-ET-1 binding to recombinant human Endothelin A receptor. | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
| Butenolide endothelin antagonists with improved aqueous solubility. |
| AID452801 | Selectivity index, ratio of Ki for DBA mouse microsome endothelin B receptor to Ki for DBA mouse microsome endothelin A receptor | 2009 | Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20
| PET-compatible endothelin receptor radioligands: synthesis and first in vitro and in vivo studies. |
| AID68338 | Antagonistic activity against human Endothelin A receptor expressed in LtK | 1995 | Journal of medicinal chemistry, Apr-14, Volume: 38, Issue:8
| Discovery of a novel series of orally active non-peptide endothelin-A (ETA) receptor-selective antagonists. |
| AID10718 | Area under the concentration-time curve from time zero to infinity in oral (5 mg/kg) fed dogs | 1997 | Journal of medicinal chemistry, Mar-28, Volume: 40, Issue:7
| Structure-activity relationships in a series of orally active gamma-hydroxy butenolide endothelin antagonists. |
| AID166795 | In vitro inhibition of ET-1 induced contraction of rabbit femoral artery rings. | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
| Butenolide endothelin antagonists with improved aqueous solubility. |
| AID574642 | Biodistribution on BALB/c mouse urine assessed as uptake index at 2.5 nmol/kg, iv after 30 mins in presence of PD156707 | 2011 | Journal of medicinal chemistry, Feb-24, Volume: 54, Issue:4
| Development and evaluation of endothelin-A receptor (radio)ligands for positron emission tomography. |
| AID66367 | Binding affinity against human cloned Endothelin B receptor expressed in CHO-K1 cells | 1997 | Journal of medicinal chemistry, Mar-28, Volume: 40, Issue:7
| Structure-activity relationships in a series of orally active gamma-hydroxy butenolide endothelin antagonists. |
| AID66202 | Inhibition of [125I]ET1 binding to rat aorta membrane Endothelin A receptor | 1998 | Bioorganic & medicinal chemistry letters, Jan-06, Volume: 8, Issue:1
| Endothelin antagonists: evaluation of 2,1,3-benzothiadiazole as a methylendioxyphenyl bioisoster. |
| AID68301 | Binding affinity against human cloned endothelin A receptor expressed in LTK-cells | 1997 | Journal of medicinal chemistry, Mar-28, Volume: 40, Issue:7
| Structure-activity relationships in a series of orally active gamma-hydroxy butenolide endothelin antagonists. |
| AID20779 | Time to reach maximum observed concentration in oral (5 mg/kg) fasted dogs | 1997 | Journal of medicinal chemistry, Mar-28, Volume: 40, Issue:7
| Structure-activity relationships in a series of orally active gamma-hydroxy butenolide endothelin antagonists. |
| AID574639 | Biodistribution on BALB/c mouse duodenum at 2.5 nmol/kg, iv after 30 mins in presence of PD156707 | 2011 | Journal of medicinal chemistry, Feb-24, Volume: 54, Issue:4
| Development and evaluation of endothelin-A receptor (radio)ligands for positron emission tomography. |
| AID68488 | Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cells | 1996 | Journal of medicinal chemistry, Mar-01, Volume: 39, Issue:5
| 2,4-Diarylpyrrolidine-3-carboxylic acids--potent ETA selective endothelin receptor antagonists. 1. Discovery of A-127722. |
| AID66545 | Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed). | 1995 | Journal of medicinal chemistry, Apr-14, Volume: 38, Issue:8
| Discovery of a novel series of orally active non-peptide endothelin-A (ETA) receptor-selective antagonists. |
| AID23580 | Mean of apparent terminal phase elimination half-life in oral (5 mg/kg) fasted dogs | 1997 | Journal of medicinal chemistry, Mar-28, Volume: 40, Issue:7
| Structure-activity relationships in a series of orally active gamma-hydroxy butenolide endothelin antagonists. |
| AID66529 | Inhibition of Endothelin B receptor mediated (ET-3) release of arachidonic acid from human cloned receptors / CHO-K1 cells | 1997 | Journal of medicinal chemistry, Mar-28, Volume: 40, Issue:7
| Structure-activity relationships in a series of orally active gamma-hydroxy butenolide endothelin antagonists. |
| AID66709 | Inhibition of [125I]ET1 binding to porcine kidney inner medulla membrane Endothelin B receptor | 1998 | Bioorganic & medicinal chemistry letters, Jan-06, Volume: 8, Issue:1
| Endothelin antagonists: evaluation of 2,1,3-benzothiadiazole as a methylendioxyphenyl bioisoster. |
| AID23581 | Mean of apparent terminal phase elimination half-life in oral (5 mg/kg) fed dogs | 1997 | Journal of medicinal chemistry, Mar-28, Volume: 40, Issue:7
| Structure-activity relationships in a series of orally active gamma-hydroxy butenolide endothelin antagonists. |
| AID66048 | Antagonism of ET-1 induced contraction of rabbit femoral artery rings (Endothelin A receptor mediated) | 1997 | Journal of medicinal chemistry, Mar-28, Volume: 40, Issue:7
| Structure-activity relationships in a series of orally active gamma-hydroxy butenolide endothelin antagonists. |
| AID66691 | Inhibitory activity against human Endothelin B receptor in chinese hamster ovary cells | 1996 | Journal of medicinal chemistry, Mar-01, Volume: 39, Issue:5
| 2,4-Diarylpyrrolidine-3-carboxylic acids--potent ETA selective endothelin receptor antagonists. 1. Discovery of A-127722. |
| AID574638 | Biodistribution on BALB/c mouse stomach at 2.5 nmol/kg, iv after 30 mins in presence of PD156707 | 2011 | Journal of medicinal chemistry, Feb-24, Volume: 54, Issue:4
| Development and evaluation of endothelin-A receptor (radio)ligands for positron emission tomography. |
| AID10717 | Area under the concentration-time curve from time zero to infinity in oral (5 mg/kg) fasted dogs | 1997 | Journal of medicinal chemistry, Mar-28, Volume: 40, Issue:7
| Structure-activity relationships in a series of orally active gamma-hydroxy butenolide endothelin antagonists. |
| AID10716 | Area under the concentration-time curve from time zero to infinity after intravenous administration of 2.5 mg/kg in dogs | 1997 | Journal of medicinal chemistry, Mar-28, Volume: 40, Issue:7
| Structure-activity relationships in a series of orally active gamma-hydroxy butenolide endothelin antagonists. |
| AID20780 | Time to reach maximum observed concentration in oral (5 mg/kg) fed dogs | 1997 | Journal of medicinal chemistry, Mar-28, Volume: 40, Issue:7
| Structure-activity relationships in a series of orally active gamma-hydroxy butenolide endothelin antagonists. |
| AID23579 | Mean of apparent terminal phase elimination half-life after intravenous administration of 2.5 mg/kg in dogs | 1997 | Journal of medicinal chemistry, Mar-28, Volume: 40, Issue:7
| Structure-activity relationships in a series of orally active gamma-hydroxy butenolide endothelin antagonists. |
| AID17945 | Absolute oral bioavailability in oral (5 mg/kg) fed dogs | 1997 | Journal of medicinal chemistry, Mar-28, Volume: 40, Issue:7
| Structure-activity relationships in a series of orally active gamma-hydroxy butenolide endothelin antagonists. |
| AID17944 | Absolute oral bioavailability in oral (5 mg/kg) fasted dogs | 1997 | Journal of medicinal chemistry, Mar-28, Volume: 40, Issue:7
| Structure-activity relationships in a series of orally active gamma-hydroxy butenolide endothelin antagonists. |
| AID574641 | Biodistribution on BALB/c mouse urine at 2.5 nmol/kg, iv after 30 mins in presence of PD156707 | 2011 | Journal of medicinal chemistry, Feb-24, Volume: 54, Issue:4
| Development and evaluation of endothelin-A receptor (radio)ligands for positron emission tomography. |
| AID176677 | Compound was evaluated for acute hypoxic pulmonary hypertension in rats | 1999 | Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
| Butenolide endothelin antagonists with improved aqueous solubility. |
| AID14096 | Maximum observed concentration in oral (5 mg/kg) fasted dogs | 1997 | Journal of medicinal chemistry, Mar-28, Volume: 40, Issue:7
| Structure-activity relationships in a series of orally active gamma-hydroxy butenolide endothelin antagonists. |
| AID452799 | Displacement of [125I]ET1 from endothelin A receptor in DBA mouse microsomes | 2009 | Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20
| PET-compatible endothelin receptor radioligands: synthesis and first in vitro and in vivo studies. |
| AID66043 | Inhibition of ET-1 induced contraction of rabbit femoral artery rings (Endothelin A receptor mediated) | 1997 | Journal of medicinal chemistry, Mar-28, Volume: 40, Issue:7
| Structure-activity relationships in a series of orally active gamma-hydroxy butenolide endothelin antagonists. |
| AID493017 | Wombat Data for BeliefDocking | 1997 | Journal of medicinal chemistry, Mar-28, Volume: 40, Issue:7
| Structure-activity relationships in a series of orally active gamma-hydroxy butenolide endothelin antagonists. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |