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Assay Detail

CHEMBL714598

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Functional
Agonistic potency towards human melanocortin 4 receptor, determined by 50% maximum cAMP release
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Melanocortin receptor 4 (CHEMBL259)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure-activity relationships of novel arylpiperazines as potent and selective agonists of the melanocortin subtype-4 receptor.
Richardson TI, Ornstein PL, Briner K, Fisher MJ, Backer RT, Biggers CK, Clay MP, Emmerson PJ, Hertel LW, Hsiung HM, Husain S, Kahl SD, Lee JA, Lindstrom TD, Martinelli MJ, Mayer JP, Mullaney JT, O'Brien TP, Pawlak JM, Revell KD, Shah J, Zgombick JM, Herr RJ, Melekhov A, Sampson PB, King CH.
J Med Chem (2004) 47 : 744 -755
PubMed 14736255 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 28 7.16 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL349850 1 8.15
CHEMBL349515 1 8.10
CHEMBL433710 1 7.85
CHEMBL423101 1 7.85
CHEMBL338594 1 7.80
CHEMBL164857 1 7.68
CHEMBL351161 1 7.47
CHEMBL349886 1 7.43
CHEMBL349887 1 7.41
CHEMBL423619 1 7.40
CHEMBL423250 1 7.36
CHEMBL353239 1 7.36
CHEMBL351088 1 7.36
CHEMBL406764 1 7.32
CHEMBL166328 1 7.15
CHEMBL164884 1 7.03
CHEMBL164671 1 7.01
CHEMBL352063 1 6.96
CHEMBL352457 1 6.85
CHEMBL352677 1 6.84
CHEMBL422027 1 6.82
CHEMBL162493 1 6.82
CHEMBL164969 1 6.70
CHEMBL167780 1 6.68
CHEMBL351400 1 6.44
CHEMBL165746 1 6.40
CHEMBL351705 1 6.31
CHEMBL349427 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL349850 EC50 = 7.0 nM 8.15
CHEMBL349515 EC50 = 8.0 nM 8.10
CHEMBL433710 EC50 = 14.0 nM 7.85
CHEMBL423101 EC50 = 14.0 nM 7.85
CHEMBL338594 EC50 = 16.0 nM 7.80
CHEMBL164857 EC50 = 21.0 nM 7.68
CHEMBL351161 EC50 = 34.0 nM 7.47
CHEMBL349886 EC50 = 37.0 nM 7.43
CHEMBL349887 EC50 = 39.0 nM 7.41
CHEMBL423619 EC50 = 40.0 nM 7.40
CHEMBL423250 EC50 = 44.0 nM 7.36
CHEMBL353239 EC50 = 44.0 nM 7.36
CHEMBL351088 EC50 = 44.0 nM 7.36
CHEMBL406764 EC50 = 48.0 nM 7.32
CHEMBL166328 EC50 = 71.0 nM 7.15
CHEMBL164884 EC50 = 93.0 nM 7.03
CHEMBL164671 EC50 = 98.0 nM 7.01
CHEMBL352063 EC50 = 110.0 nM 6.96
CHEMBL352457 EC50 = 140.0 nM 6.85
CHEMBL352677 EC50 = 145.0 nM 6.84
CHEMBL422027 EC50 = 150.0 nM 6.82
CHEMBL162493 EC50 = 150.0 nM 6.82
CHEMBL164969 EC50 = 200.0 nM 6.70
CHEMBL167780 EC50 = 210.0 nM 6.68
CHEMBL351400 EC50 = 360.0 nM 6.44
CHEMBL165746 EC50 = 400.0 nM 6.40
CHEMBL351705 EC50 = 490.0 nM 6.31
CHEMBL349427 EC50 = 1300.0 nM 5.89