| Assay ID | Title | Year | Journal | Article |
|---|
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
| Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
| Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID347093 | Oral bioavailability in Beagle dog | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate. |
| AID347521 | Tmax in Sprague-Dawley rat at 5 mg/kg, po | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate. |
| AID347504 | Half life in rabbit gastric antrum native tissue at 3 uM | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate. |
| AID347514 | Inhibition of human CYP3A4 expressed in Escherichia coli using 7BQ substrate by time dependent inhibition assay | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate. |
| AID347516 | Potentiation of electric field stimulated-rabbit gastric antrum contraction at 3 uM | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate. |
| AID347520 | Cmax in Sprague-Dawley rat at 5 mg/kg, po | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate. |
| AID347096 | Inhibition of human CYP2C19 | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate. |
| AID1889090 | Agonist activity at rabbit GPR38 expressed in COS-7 cells | 2022 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 59 | Discovery of DS-3801b, a non-macrolide GPR38 agonist with N-methylanilide structure. |
| AID347506 | Agonist activity at human recombinant motilin receptor expressed in CHO cells assessed as increase in intracellular calcium by FLIPR assay | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate. |
| AID347515 | Inhibition of human CYP3A4 expressed in Escherichia coli using diethoxyfluorescein substrate assessed as decrease in enzyme activity by time dependent inhibition assay | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate. |
| AID347101 | Protein binding in rat plasma | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate. |
| AID1889093 | Ex vivo agonist activity at GPR38 in rabbit duodenum muscle tissue assessed as intestinal contractile activity | 2022 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 59 | Discovery of DS-3801b, a non-macrolide GPR38 agonist with N-methylanilide structure. |
| AID347513 | Inhibition of human CYP3A4 expressed in Escherichia coli using diethoxyfluorescein substrate by time dependent inhibition assay | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate. |
| AID347507 | Intrinsic clearance in human | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate. |
| AID347094 | Inhibition of human CYP1A2 | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate. |
| AID347100 | Protein binding in human plasma | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate. |
| AID347098 | Agonist activity at human Ghrelin receptor | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate. |
| AID347518 | Potentiation of electric field stimulated-rabbit gastric antrum contraction at 0.3 uM | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate. |
| AID347519 | Potentiation of electric field stimulated-rabbit gastric antrum contraction at 0.1 uM | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate. |
| AID347517 | Potentiation of electric field stimulated-rabbit gastric antrum contraction at 1 uM | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate. |
| AID347092 | Oral bioavailability in Sprague-Dawley rat | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate. |
| AID347099 | Binding affinity to human ERG | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate. |
| AID347095 | Inhibition of human CYP2C9 | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate. |
| AID347508 | Intrinsic clearance in Sprague-Dawley rat | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate. |
| AID347512 | Intrinsic activity at human recombinant motilin receptor expressed in CHO cells relative to motilin | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate. |
| AID347522 | AUC (0 to t) in Sprague-Dawley rat at 5 mg/kg, po | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate. |
| AID1889088 | Agonist activity at human GPR38 expressed in COS-7 cells | 2022 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 59 | Discovery of DS-3801b, a non-macrolide GPR38 agonist with N-methylanilide structure. |
| AID347097 | Inhibition of human CYP2D6 | 2009 | Journal of medicinal chemistry, Feb-26, Volume: 52, Issue:4
| Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate. |
| AID1346284 | Human motilin receptor (Motilin receptor) | 2015 | Expert opinion on investigational drugs, Jan, Volume: 24, Issue:1
| The investigational drug camicinal for the treatment of gastroparesis. |
| AID1346284 | Human motilin receptor (Motilin receptor) | 2009 | Neurogastroenterology and motility, Jun, Volume: 21, Issue:6
| GSK962040: a small molecule, selective motilin receptor agonist, effective as a stimulant of human and rabbit gastrointestinal motility. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |