Ki Summary

Reaction Details

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Target

Galanin receptor type 1

Ligand

BDBM85072

Substrate

n/a

0.60±n/a nM

Comments

PDSP_864

Citation

Smith, KE; Walker, MW; Artymyshyn, R; Bard, J; Borowsky, B; Tamm, JA; Yao, WJ; Vaysse, PJ; Branchek, TA; Gerald, C; Jones, KA Cloned human and rat galanin GALR3 receptors. Pharmacology and activation of G-protein inwardly rectifying K+ channels. J Biol Chem 273:23321-6 (1998) [PubMed] Article

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Target

Name:

Galanin receptor type 1

Synonyms:

Type:

Enzyme Catalytic Domain

Mol. Mass.:

38883.91

Organism:

RAT

Description:

Galanin R1 GALR1 RAT::Q62805

Residue:

346

Sequence:

MELAPVNLSEGNGSDPEPPAEPRPLFGIGVENFITLVVFGLIFAMGVLGNSLVITVLARSKPGKPRSTTNLFILNLSIADLAYLLFCIPFQATVYALPTWVLGAFICKFIHYFFTVSMLVSIFTLAAMSVDRYVAIVHSRRSSSLRVSRNALLGVGFIWALSIAMASPVAYYQRLFHRDSNQTFCWEHWPNQLHKKAYVVCTFVFGYLLPLLLICFCYAKVLNHLHKKLKNMSKKSEASKKKTAQTVLVVVVVFGISWLPHHVIHLWAEFGAFPLTPASFFFRITAHCLAYSNSSVNPIIYAFLSENFRKAYKQVFKCRVCNESPHGDAKEKNRIDTPPSTNCTHV

Inhibitor

Name:

BDBM85072

Synonyms:

Galanin, Human

Type:

Small organic molecule

Emp. Form.:

C139H210N42O43

Mol. Mass.:

3157.4103

SMILES:

CC(C)C[C@H](NC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CC(N)=O)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CN)[C@@H](C)O)C(C)C)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(O)=O |wU:212.220,131.139,139.152,71.79,166.175,182.187,54.57,211.217,20.25,37.39,112.114,97.99,155.160,wD:202.210,102.111,123.131,93.95,81.87,174.183,160.167,60.68,186.203,4.4,12.16,43.51,29.33,218.224,(13.66,18.44,;13.66,16.9,;12.32,16.13,;14.99,16.13,;14.99,14.59,;16.32,13.82,;17.86,14.59,;17.86,16.13,;19.2,13.82,;20.53,14.59,;22.07,13.82,;22.07,12.28,;23.4,14.59,;23.4,16.13,;22.07,16.9,;22.07,18.44,;20.74,16.13,;24.74,13.82,;26.28,14.59,;26.28,16.13,;27.61,13.82,;27.61,12.28,;28.95,11.51,;28.95,9.97,;30.28,9.2,;31.61,9.97,;28.95,14.59,;30.49,13.82,;30.49,12.28,;31.82,14.59,;31.82,16.13,;33.15,16.9,;33.15,18.44,;34.49,16.13,;33.15,13.82,;32.43,3.03,;32.43,1.49,;31.1,3.8,;31.1,5.34,;32.43,6.11,;29.76,3.03,;28.22,3.8,;28.22,5.34,;26.89,3.03,;26.89,1.49,;28.22,.72,;28.22,-.82,;29.56,-1.59,;30.89,-.82,;30.89,.72,;29.56,1.49,;25.56,3.8,;24.02,3.03,;24.02,1.49,;22.68,3.8,;22.68,5.34,;24.02,6.11,;21.35,3.03,;19.81,3.8,;19.81,5.34,;18.47,3.03,;18.47,1.49,;19.81,.72,;19.81,-.82,;21.14,-1.59,;22.48,-.82,;23.81,-1.59,;22.48,.72,;17.14,3.8,;15.6,3.03,;15.6,1.49,;14.27,3.8,;14.27,5.34,;15.6,6.11,;17.01,5.49,;18.04,6.63,;17.27,7.97,;15.76,7.65,;12.93,3.03,;11.39,3.8,;11.39,5.34,;10.06,3.03,;10.06,1.49,;11.39,.72,;11.39,-.82,;12.73,1.49,;8.73,3.8,;7.19,3.03,;7.19,1.49,;5.85,3.8,;4.52,3.03,;5.24,-7.75,;5.24,-9.29,;6.57,-6.98,;7.91,-7.75,;9.45,-6.98,;9.45,-5.44,;10.78,-7.75,;10.78,-9.29,;12.12,-6.98,;13.66,-7.75,;13.66,-9.29,;14.99,-6.98,;14.99,-5.44,;13.66,-4.67,;12.25,-5.29,;11.22,-4.15,;11.99,-2.81,;13.49,-3.13,;16.32,-7.75,;17.66,-6.98,;17.66,-5.44,;18.99,-7.75,;19.15,-9.28,;20.66,-9.6,;21.43,-8.26,;20.4,-7.12,;20.72,-5.61,;19.57,-4.58,;22.18,-5.14,;23.33,-6.17,;24.79,-5.69,;25.11,-4.19,;25.94,-6.72,;27.4,-6.25,;27.72,-4.74,;29.19,-4.26,;26.58,-3.71,;25.62,-8.23,;26.76,-9.26,;28.22,-8.78,;26.44,-10.77,;24.98,-11.24,;24.65,-12.75,;23.19,-13.22,;25.8,-13.78,;27.58,-11.8,;29.05,-11.32,;29.37,-9.81,;30.19,-12.35,;29.87,-13.86,;31.02,-14.89,;30.7,-16.39,;31.84,-17.42,;33.31,-16.95,;34.45,-17.98,;33.63,-15.44,;32.48,-14.41,;31.66,-11.87,;31.98,-10.37,;30.83,-9.34,;33.44,-9.89,;33.76,-8.39,;35.23,-7.91,;35.55,-6.4,;36.37,-8.94,;36.05,-10.45,;37.84,-8.46,;38.98,-9.49,;38.66,-11,;40.45,-9.02,;40.77,-7.51,;42.23,-7.04,;41.59,-10.05,;43.06,-9.57,;43.38,-8.07,;44.2,-10.6,;43.88,-12.11,;45.02,-13.14,;44.7,-14.65,;46.49,-12.66,;45.66,-10.13,;45.98,-8.62,;44.84,-7.59,;47.45,-8.15,;47.77,-6.64,;46.62,-5.61,;46.94,-4.1,;45.16,-6.08,;48.59,-9.18,;50.06,-8.7,;50.38,-7.19,;51.2,-9.73,;52.67,-9.25,;53.81,-10.29,;53.49,-11.79,;55.28,-9.81,;55.6,-8.3,;57.06,-7.83,;58.3,-8.73,;59.54,-7.83,;59.07,-6.37,;59.85,-5.04,;59.08,-3.71,;57.54,-3.7,;56.77,-5.04,;57.53,-6.37,;56.42,-10.84,;56.1,-12.35,;54.64,-12.82,;57.25,-13.38,;56.93,-14.88,;50.88,-11.24,;49.42,-11.71,;52.03,-12.27,;6.57,-5.44,;5.24,-4.67,;7.91,-4.67,;13.66,13.82,;13.66,12.28,;12.12,14.59,;10.78,13.82,;10.78,12.28,;12.12,11.51,;9.45,11.51,;9.45,14.59,;9.45,16.13,;7.91,13.82,;6.57,14.59,;6.57,16.13,;5.24,16.9,;5.24,13.82,;3.91,14.59,;5.24,12.28,)|

Structure: