| Reaction Details |
|---|
| Report a problem with these data |
| Target | Vanilloid Receptor 1 (TRPV1, VR1) |
|---|
| Ligand | A-778317 |
|---|
| Substrate/Competitor | Radiolabeled A-778317 |
|---|
| Meas. Tech. | Radioligand Binding Assay and Antagonist Ca2+ Influx Functional Assay |
|---|
| pH | 7.4±n/a |
|---|
| Temperature | 298.15±n/a K |
|---|
| Ki | 7±1 nM |
|---|
| EC50 | 5±2 nM |
|---|
| Citation |  Bianchi, BR; El Kouhen, R; Neelands, TR; Lee, CH; Gomtsyan, A; Raja, SN; Vaidyanathan, SN; Surber, B; McDonald, HA; Surowy, CS; Faltynek, CR; Moreland, RB; Jarvis, MF; Puttfarcken, PS [3H]A-778317 [1-((R)-5-tert-butyl-indan-1-yl)-3-isoquinolin-5-yl-urea]: a novel, stereoselective, high-affinity antagonist is a useful radioligand for the human transient receptor potential vanilloid-1 (TRPV1) receptor.J Pharmacol Exp Ther.323:285-93(2007)[PubMed] |
|---|
| More Info. |
Get all data from this article
, Inhibition_Run data
, Solution Info
, Assay Method
|
|---|
| Vanilloid Receptor 1 (TRPV1, VR1) |
|---|
| Name | Vanilloid Receptor 1 (TRPV1, VR1) |
|---|
| Synonyms | Capsaicin receptor | Transient receptor potential cation channel subfamily V member 1 | osm-9-like TRP channel 1 | OTRPC1 | Vanilloid receptor type 1-like |
|---|
| Type | Transient Receptor |
|---|
| Mol. Mass. | 94938 |
|---|
| Organism | Homo sapiens (human) |
|---|
| Description | VR1-transfected cells were used in the assay. |
|---|
| Residue | 839 |
|---|
| Sequence | MKKWSSTDLGAAADPLQKDTCPDPLDGDPNSRPPPAKPQLSTAKSRTRLFGKGDSEEAFP
VDCPHEEGELDSCPTITVSPVITIQRPGDGPTGARLLSQDSVAASTEKTLRLYDRRSIFE
AVAQNNCQDLESLLLFLQKSKKHLTDNEFKDPETGKTCLLKAMLNLHDGQNTTIPLLLEI
ARQTDSLKELVNASYTDSYYKGQTALHIAIERRNMALVTLLVENGADVQAAAHGDFFKKT
KGRPGFYFGELPLSLAACTNQLGIVKFLLQNSWQTADISARDSVGNTVLHALVEVADNTA
DNTKFVTSMYNEILILGAKLHPTLKLEELTNKKGMTPLALAAGTGKIGVLAYILQREIQE
PECRHLSRKFTEWAYGPVHSSLYDLSCIDTCEKNSVLEVIAYSSSETPNRHDMLLVEPLN
RLLQDKWDRFVKRIFYFNFLVYCLYMIIFTMAAYYRPVDGLPPFKMEKTGDYFRVTGEIL
SVLGGVYFFFRGIQYFLQRRPSMKTLFVDSYSEMLFFLQSLFMLATVVLYFSHLKEYVAS
MVFSLALGWTNMLYYTRGFQQMGIYAVMIEKMILRDLCRFMFVYIVFLFGFSTAVVTLIE
DGKNDSLPSESTSHRWRGPACRPPDSSYNSLYSTCLELFKFTIGMGDLEFTENYDFKAVF
IILLLAYVILTYILLLNMLIALMGETVNKIAQESKNIWKLQRAITILDTEKSFLKCMRKA
FRSGKLLQVGYTPDGKDDYRWCFRVDEVNWTTWNTNVGIINEDPGNCEGVKRTLSFSLRS
SRVSGRHWKNFALVPLLREASARDRQSAQPEEVYLRQFSGSLKPEDAEVFKSPAASGEK
| |
|
|---|
| A-778317 |
|---|
| Name | A-778317 |
|---|
| Synonyms: | 3-[(1R)-5-tert-butyl-2,3-dihydro-1H-inden-1-yl]-1-isoquinolin-5-ylurea |
|---|
| Type | Small organic molecule |
|---|
| Emp. Form. | C23H25N3O |
|---|
| Mol. Mass. | 359.4641 |
|---|
| SMILES | CC(C)(C)c1ccc2[C@@H](CCc2c1)NC(=O)Nc1cccc2cnccc12 |r| |
|---|
| Structure | |
|---|
| Radiolabeled A-778317 |
|---|
| Name | Radiolabeled A-778317 |
|---|
| Synonyms: | 1-[(1R)-5-tert-butyl-2,3-dihydro-1H-inden-1-yl]-3-isoquinolin-5-ylurea | 3-[(1R)-5-tert-butyl-2,3-dihydro-1H-inden-1-yl]-1-isoquinolin-5-ylurea | [3H] A-778317 |
|---|
| Type | Small organic molecule |
|---|
| Emp. Form. | C23H25N3O |
|---|
| Mol. Mass. | 359.4641 |
|---|
| SMILES | CC(C)(C)c1ccc2[C@@H](CCc2c1)NC(=O)Nc1cccc2cnccc12 |r| |
|---|
| Structure | |
|---|