[
{
"interactionId": 3205,
"targetId": 282,
"targetName": "MC1 receptor",
"ligandAsTargetId": 0,
"targetSpecies": "Human",
"primaryTarget": false,
"targetBindingSite": "",
"ligandId": 1326,
"ligandName": "[125I]NDP-MSH",
"ligandContext": "",
"endogenous": false,
"type": "Agonist",
"action": "Full agonist",
"actionComment": "",
"selectivity": "Not Determined",
"concentrationRange": "",
"affinity": "9.5",
"affinityParameter": "pKd",
"originalAffinity": "3.3x10-10",
"originalAffinityType": "Kd",
"originalAffinityRelation": "=",
"assayDescription": "",
"assayConditions": "",
"useDependent": false,
"voltageDependent": false,
"voltage": "",
"physiologicalVoltage": false,
"conciseView": true,
"refs": [
{
"referenceId": 4333,
"pmid": 15840392,
"type": "Journal",
"title": "Eur J Pharmacol",
"year": 2005,
"volume": "512",
"issue": "2-3",
"pages": "85-95",
"articleTitle": "Co-operative regulation of ligand binding to melanocortin receptor subtypes: evidence for interacting binding sites.",
"authors": "Kopanchuk S, Veiksina S, Petrovska R, Mutule I, Szardenings M, Rinken A, Wikberg JE"
}
]
},
{
"interactionId": 79720,
"targetId": 282,
"targetName": "MC1 receptor",
"ligandAsTargetId": 0,
"targetSpecies": "Human",
"primaryTarget": false,
"targetBindingSite": "",
"ligandId": 3633,
"ligandName": "ACTH",
"ligandContext": "",
"endogenous": false,
"type": "Agonist",
"action": "Agonist",
"actionComment": "",
"selectivity": "Not Determined",
"concentrationRange": "",
"affinity": "8.6",
"affinityParameter": "pKi",
"originalAffinity": "2.5x10-9",
"originalAffinityType": "Ki",
"originalAffinityRelation": "=",
"assayDescription": "",
"assayConditions": "",
"useDependent": false,
"voltageDependent": false,
"voltage": "",
"physiologicalVoltage": false,
"conciseView": false,
"refs": [
{
"referenceId": 4375,
"pmid": 7774675,
"type": "Journal",
"title": "Eur J Pharmacol",
"year": 1995,
"volume": "288",
"issue": "3",
"pages": "311-317",
"articleTitle": "Characterisation of melanocortin receptor subtypes by radioligand binding analysis.",
"authors": "Schioth HB, Muceniece R, Wikberg JE, Chhajlani V",
"pubStatus": ""
}
]
},
{
"interactionId": 83756,
"targetId": 282,
"targetName": "MC1 receptor",
"ligandAsTargetId": 0,
"targetSpecies": "Human",
"primaryTarget": false,
"targetBindingSite": "",
"ligandId": 9272,
"ligandName": "setmelanotide",
"ligandContext": "",
"endogenous": false,
"type": "Agonist",
"action": "Agonist",
"actionComment": "",
"selectivity": "Not Determined",
"concentrationRange": "",
"affinity": "8.4",
"affinityParameter": "pKi",
"originalAffinity": "3.9x10-9",
"originalAffinityType": "Ki",
"originalAffinityRelation": "=",
"assayDescription": "",
"assayConditions": "",
"useDependent": false,
"voltageDependent": false,
"voltage": "",
"physiologicalVoltage": false,
"conciseView": false,
"refs": [
{
"referenceId": 31400,
"pmid": 19646498,
"type": "Journal",
"title": "Peptides",
"year": 2009,
"volume": "30",
"issue": "10",
"pages": "1892-900",
"articleTitle": "Analysis of the therapeutic functions of novel melanocortin receptor agonists in MC3R- and MC4R-deficient C57BL/6J mice.",
"authors": "Kumar KG, Sutton GM, Dong JZ, Roubert P, Plas P, Halem HA, Culler MD, Yang H, Dixit VD, Butler AA",
"pubStatus": ""
}
]
},
{
"interactionId": 86505,
"targetId": 282,
"targetName": "MC1 receptor",
"ligandAsTargetId": 0,
"targetSpecies": "Human",
"primaryTarget": false,
"targetBindingSite": "",
"ligandId": 10408,
"ligandName": "bremelanotide",
"ligandContext": "",
"endogenous": false,
"type": "Agonist",
"action": "Agonist",
"actionComment": "",
"selectivity": "Not Determined",
"concentrationRange": "",
"affinity": "8.2",
"affinityParameter": "pKi",
"originalAffinity": "6.4x10-9",
"originalAffinityType": "Ki",
"originalAffinityRelation": "=",
"assayDescription": "Inhibition of 125I-NDP-αMSH binding to membranes from BHK570 cells stably expressing human MC1 receptor.",
"assayConditions": "",
"useDependent": false,
"voltageDependent": false,
"voltage": "",
"physiologicalVoltage": false,
"conciseView": false,
"refs": [
{
"referenceId": 37855,
"pmid": 22335602,
"type": "Journal",
"title": "J Med Chem",
"year": 2012,
"volume": "55",
"issue": "5",
"pages": "1969-77",
"articleTitle": "Identification and in vivo and in vitro characterization of long acting and melanocortin 4 receptor (MC4-R) selective α-melanocyte-stimulating hormone (α-MSH) analogues.",
"authors": "Conde-Frieboes K, Thøgersen H, Lau JF, Sensfuss U, Hansen TK, Christensen L, Spetzler J, Olsen HB, Nilsson C, Raun K et al.",
"pubStatus": "",
"doi": ""
}
]
},
{
"interactionId": 3199,
"targetId": 282,
"targetName": "MC1 receptor",
"ligandAsTargetId": 0,
"targetSpecies": "Human",
"primaryTarget": false,
"ligandId": 1320,
"ligandName": "α-MSH",
"endogenous": true,
"type": "Agonist",
"action": "Full agonist",
"concentrationRange": "",
"affinity": "8.4",
"affinityParameter": "pIC50",
"originalAffinity": "",
"originalAffinityType": "",
"originalAffinityRelation": "",
"useDependent": false,
"voltageDependent": false,
"voltage": "",
"physiologicalVoltage": false,
"conciseView": false,
"refs": [
{
"referenceId": 4327,
"pmid": 12007532,
"type": "Journal",
"title": "Eur J Pharmacol",
"year": 2002,
"volume": "440",
"issue": "2-3",
"pages": "141-57",
"articleTitle": "The role of melanocortins in body weight regulation: opportunities for the treatment of obesity.",
"authors": "MacNeil DJ, Howard AD, Guan X, Fong TM, Nargund RP, Bednarek MA, Goulet MT, Weinberg DH, Strack AM, Marsh DJ et al."
}
]
},
{
"interactionId": 3200,
"targetId": 282,
"targetName": "MC1 receptor",
"ligandAsTargetId": 0,
"targetSpecies": "Human",
"primaryTarget": false,
"ligandId": 1321,
"ligandName": "HS014",
"endogenous": false,
"type": "Agonist",
"action": "Partial agonist",
"concentrationRange": "",
"affinity": "7.0",
"affinityParameter": "pKd",
"originalAffinity": "",
"originalAffinityType": "",
"originalAffinityRelation": "",
"useDependent": false,
"voltageDependent": false,
"voltage": "",
"physiologicalVoltage": false,
"conciseView": false,
"refs": [
{
"referenceId": 4328,
"pmid": 10657491,
"type": "Journal",
"title": "Neuropeptides",
"year": 1999,
"volume": "33",
"issue": "3",
"pages": "191-6",
"articleTitle": "Further pharmacological characterization of the selective melanocortin 4 receptor antagonist HS014: comparison with SHU9119.",
"authors": "Schiöth HB, Muceniece R, Mutulis F, Bouifrouri AA, Mutule I, Wikberg JE"
}
]
},
{
"interactionId": 3201,
"targetId": 282,
"targetName": "MC1 receptor",
"ligandAsTargetId": 0,
"targetSpecies": "Human",
"primaryTarget": false,
"ligandId": 1322,
"ligandName": "MS05",
"endogenous": false,
"type": "Agonist",
"action": "Full agonist",
"concentrationRange": "",
"affinity": "9.1",
"affinityParameter": "pKd",
"originalAffinity": "",
"originalAffinityType": "",
"originalAffinityRelation": "",
"useDependent": false,
"voltageDependent": false,
"voltage": "",
"physiologicalVoltage": false,
"conciseView": false,
"refs": [
{
"referenceId": 4329,
"pmid": 10764951,
"type": "Journal",
"title": "Peptides",
"year": 2000,
"volume": "21",
"issue": "2",
"pages": "239-43",
"articleTitle": "New highly specific agonistic peptides for human melanocortin MC(1) receptor.",
"authors": "Szardenings M, Muceniece R, Mutule I, Mutulis F, Wikberg JE"
}
]
},
{
"interactionId": 3202,
"targetId": 282,
"targetName": "MC1 receptor",
"ligandAsTargetId": 0,
"targetSpecies": "Human",
"primaryTarget": false,
"ligandId": 1323,
"ligandName": "MT-II",
"endogenous": false,
"type": "Agonist",
"action": "Full agonist",
"concentrationRange": "",
"affinity": "9.4",
"affinityParameter": "pIC50",
"originalAffinity": "",
"originalAffinityType": "",
"originalAffinityRelation": "",
"useDependent": false,
"voltageDependent": false,
"voltage": "",
"physiologicalVoltage": false,
"conciseView": false,
"refs": [
{
"referenceId": 4327,
"pmid": 12007532,
"type": "Journal",
"title": "Eur J Pharmacol",
"year": 2002,
"volume": "440",
"issue": "2-3",
"pages": "141-57",
"articleTitle": "The role of melanocortins in body weight regulation: opportunities for the treatment of obesity.",
"authors": "MacNeil DJ, Howard AD, Guan X, Fong TM, Nargund RP, Bednarek MA, Goulet MT, Weinberg DH, Strack AM, Marsh DJ et al."
},
{
"referenceId": 4330,
"pmid": 2535874,
"type": "Journal",
"title": "J Med Chem",
"year": 1989,
"volume": "32",
"pages": "174-179",
"articleTitle": "Design of potent linear α-melanotropin 4-10 analogues modified in positions 5 and 10.",
"authors": "Al-Obeidi F, Hruby VJ, Castrucci AM, Hadley ME"
}
]
},
{
"interactionId": 3203,
"targetId": 282,
"targetName": "MC1 receptor",
"ligandAsTargetId": 0,
"targetSpecies": "Human",
"primaryTarget": false,
"ligandId": 1324,
"ligandName": "afamelanotide",
"endogenous": false,
"type": "Agonist",
"action": "Full agonist",
"concentrationRange": "",
"affinity": "10.0",
"affinityParameter": "pIC50",
"originalAffinity": "",
"originalAffinityType": "",
"originalAffinityRelation": "",
"useDependent": false,
"voltageDependent": false,
"voltage": "",
"physiologicalVoltage": false,
"conciseView": false,
"refs": [
{
"referenceId": 4327,
"pmid": 12007532,
"type": "Journal",
"title": "Eur J Pharmacol",
"year": 2002,
"volume": "440",
"issue": "2-3",
"pages": "141-57",
"articleTitle": "The role of melanocortins in body weight regulation: opportunities for the treatment of obesity.",
"authors": "MacNeil DJ, Howard AD, Guan X, Fong TM, Nargund RP, Bednarek MA, Goulet MT, Weinberg DH, Strack AM, Marsh DJ et al."
},
{
"referenceId": 4331,
"pmid": 3286233,
"type": "Journal",
"title": "Endocr Rev",
"year": 1988,
"volume": "9",
"pages": "159-179",
"articleTitle": "Proopiomelanocortin processing in the pituitary, central nervous system, and peripheral tissues.",
"authors": "Smith AI, Funder JW"
}
]
},
{
"interactionId": 3204,
"targetId": 282,
"targetName": "MC1 receptor",
"ligandAsTargetId": 0,
"targetSpecies": "Human",
"primaryTarget": false,
"ligandId": 1325,
"ligandName": "SHU9119",
"endogenous": false,
"type": "Agonist",
"action": "Partial agonist",
"concentrationRange": "",
"affinity": "9.2",
"affinityParameter": "pKd",
"originalAffinity": "",
"originalAffinityType": "",
"originalAffinityRelation": "",
"useDependent": false,
"voltageDependent": false,
"voltage": "",
"physiologicalVoltage": false,
"conciseView": false,
"refs": [
{
"referenceId": 4328,
"pmid": 10657491,
"type": "Journal",
"title": "Neuropeptides",
"year": 1999,
"volume": "33",
"issue": "3",
"pages": "191-6",
"articleTitle": "Further pharmacological characterization of the selective melanocortin 4 receptor antagonist HS014: comparison with SHU9119.",
"authors": "Schiöth HB, Muceniece R, Mutulis F, Bouifrouri AA, Mutule I, Wikberg JE"
},
{
"referenceId": 4332,
"pmid": 7658432,
"type": "Journal",
"title": "J Med Chem",
"year": 1995,
"volume": "38",
"issue": "18",
"pages": "3454-61",
"articleTitle": "Cyclic lactam alpha-melanotropin analogues of Ac-Nle4-cyclo[Asp5, D-Phe7,Lys10] alpha-melanocyte-stimulating hormone-(4-10)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin receptors.",
"authors": "Hruby VJ, Lu D, Sharma SD, Castrucci AL, Kesterson RA, al-Obeidi FA, Hadley ME, Cone RD"
}
]
},
{
"interactionId": 3206,
"targetId": 282,
"targetName": "MC1 receptor",
"ligandAsTargetId": 0,
"targetSpecies": "Human",
"primaryTarget": false,
"ligandId": 1327,
"ligandName": "ASIP [90-132 (L89Y)]",
"endogenous": false,
"type": "Antagonist",
"action": "Inverse agonist",
"concentrationRange": "",
"affinity": "8.1",
"affinityParameter": "pIC50",
"originalAffinity": "",
"originalAffinityType": "",
"originalAffinityRelation": "",
"useDependent": false,
"voltageDependent": false,
"voltage": "",
"physiologicalVoltage": false,
"conciseView": false,
"refs": [
{
"referenceId": 4317,
"pmid": 11705773,
"type": "Journal",
"title": "Am J Physiol Regul Integr Comp Physiol",
"year": 2001,
"volume": "281",
"issue": "6",
"pages": "R1877-86",
"articleTitle": "Functional properties of an agouti signaling protein variant and characteristics of its cognate radioligand.",
"authors": "Yang YK, Dickinson C, Lai YM, Li JY, Gantz I"
},
{
"referenceId": 4334,
"pmid": 9058374,
"type": "Journal",
"title": "Mol Endocrinol",
"year": 1997,
"volume": "11",
"issue": "3",
"pages": "274-80",
"articleTitle": "Effects of recombinant agouti-signaling protein on melanocortin action.",
"authors": "Yang YK, Ollmann MM, Wilson BD, Dickinson C, Yamada T, Barsh GS, Gantz I"
}
]
},
{
"interactionId": 3207,
"targetId": 282,
"targetName": "MC1 receptor",
"ligandAsTargetId": 0,
"targetSpecies": "Human",
"primaryTarget": false,
"ligandId": 1328,
"ligandName": "HS024",
"endogenous": false,
"type": "Antagonist",
"action": "Antagonist",
"concentrationRange": "",
"affinity": "7.7",
"affinityParameter": "pKd",
"originalAffinity": "",
"originalAffinityType": "",
"originalAffinityRelation": "",
"useDependent": false,
"voltageDependent": false,
"voltage": "",
"physiologicalVoltage": false,
"conciseView": false,
"refs": [
{
"referenceId": 4335,
"pmid": 9832440,
"type": "Journal",
"title": "Endocrinology",
"year": 1998,
"volume": "139",
"issue": "12",
"pages": "5006-14",
"articleTitle": "Discovery of a novel superpotent and selective melanocortin-4 receptor antagonist (HS024): evaluation in vitro and in vivo.",
"authors": "Kask A, Mutulis F, Muceniece R, Pähkla R, Mutule I, Wikberg JE, Rägo L, Schiöth HB"
}
]
}
]