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Assay Detail

CHEMBL838103

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Effective dose against cAMP accumulation
28
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

1-Amino-1,2,3,4-tetrahydronaphthalene-2-carboxylic acid as a Tic mimetic: application in the synthesis of potent human melanocortin-4 receptor selective agonists.
Bakshi RK, Hong Q, Olson JT, Ye Z, Sebhat IK, Weinberg DH, MacNeil T, Kalyani RN, Tang R, Martin WJ, Strack A, McGowan E, Tamvakopoulos C, Miller RR, Stearns RA, Tang W, Maclntyre DE, van der Ploeg LH, Patchett AA, Nargund RP.
Bioorg Med Chem Lett (2005) 15 : 3430 -3433
PubMed 15951175 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 28 6.93 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL360819 4 8.82
CHEMBL433764 4 8.72
CHEMBL339053 4 8.68
CHEMBL362523 4 8.48
CHEMBL360818 4 8.15
CHEMBL2113041 4 7.77
CHEMBL187990 4 7.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL360819 EC50 = 1.5 nM 8.82
CHEMBL433764 EC50 = 1.9 nM 8.72
CHEMBL339053 EC50 = 2.1 nM 8.68
CHEMBL362523 EC50 = 3.3 nM 8.48
CHEMBL360818 EC50 = 7.1 nM 8.15
CHEMBL2113041 EC50 = 17.0 nM 7.77
CHEMBL187990 EC50 = 21.0 nM 7.68
CHEMBL360818 EC50 = 99.0 nM 7.00
CHEMBL187990 EC50 = 110.0 nM 6.96
CHEMBL360818 EC50 = 130.0 nM 6.89
CHEMBL360819 EC50 = 140.0 nM 6.85
CHEMBL362523 EC50 = 150.0 nM 6.82
CHEMBL187990 EC50 = 180.0 nM 6.75
CHEMBL362523 EC50 = 200.0 nM 6.70
CHEMBL433764 EC50 = 250.0 nM 6.60
CHEMBL2113041 EC50 = 280.0 nM 6.55
CHEMBL360818 EC50 = 280.0 nM 6.55
CHEMBL360819 EC50 = 390.0 nM 6.41
CHEMBL362523 EC50 = 430.0 nM 6.37
CHEMBL339053 EC50 = 737.0 nM 6.13
CHEMBL433764 EC50 = 780.0 nM 6.11
CHEMBL2113041 EC50 = 800.0 nM 6.10
CHEMBL360819 EC50 = 960.0 nM 6.02
CHEMBL187990 EC50 = 1000.0 nM 6.00
CHEMBL339053 EC50 = 2487.0 nM 5.60
CHEMBL339053 EC50 = 2850.0 nM 5.54
CHEMBL433764 EC50 - nM -
CHEMBL2113041 EC50 - nM -