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Assay Detail

CHEMBL833834

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

Functional
Antagonist activity towards alpha-MSH stimulated accumulation of cAMP in HEK 293 cells
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 1 — Organism
Curated By Intermediate

Target

HEK293 (CHEMBL614818)
Type CELL-LINE
Organism Homo sapiens

Publication

Identification of agonists and antagonists of the human melanocortin-4 receptor from piperazinebenzylamines.
Tran JA, Pontillo J, Arellano M, White NS, Fleck BA, Marinkovic D, Tucci FC, Lanier M, Nelson J, Saunders J, Foster AC, Chen C.
Bioorg Med Chem Lett (2005) 15 : 833 -837
PubMed 15664867 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 24 6.55 8.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL360716 1 8.33
CHEMBL182277 1 7.51
CHEMBL341982 1 7.40
CHEMBL2113023 1 6.68
CHEMBL182900 1 6.68
CHEMBL181788 1 6.66
CHEMBL362841 1 6.64
CHEMBL368023 1 6.48
CHEMBL183610 1 6.46
CHEMBL2113020 1 6.44
CHEMBL366706 1 6.44
CHEMBL360296 1 6.44
CHEMBL2113019 1 6.41
CHEMBL369104 1 6.40
CHEMBL362850 1 6.36
CHEMBL366708 1 6.28
CHEMBL368022 1 6.26
CHEMBL180545 1 6.25
CHEMBL180304 1 6.24
CHEMBL369348 1 6.24
CHEMBL183134 1 6.20
CHEMBL181277 1 6.19
CHEMBL2113022 1 6.14
CHEMBL183114 1 6.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL360716 EC50 = 4.7 nM 8.33
CHEMBL182277 EC50 = 31.0 nM 7.51
CHEMBL341982 EC50 = 40.0 nM 7.40
CHEMBL2113023 EC50 = 210.0 nM 6.68
CHEMBL182900 EC50 = 210.0 nM 6.68
CHEMBL181788 EC50 = 220.0 nM 6.66
CHEMBL362841 EC50 = 230.0 nM 6.64
CHEMBL368023 EC50 = 330.0 nM 6.48
CHEMBL183610 EC50 = 350.0 nM 6.46
CHEMBL2113020 EC50 = 360.0 nM 6.44
CHEMBL366706 EC50 = 360.0 nM 6.44
CHEMBL360296 EC50 = 360.0 nM 6.44
CHEMBL2113019 EC50 = 390.0 nM 6.41
CHEMBL369104 EC50 = 400.0 nM 6.40
CHEMBL362850 EC50 = 440.0 nM 6.36
CHEMBL366708 EC50 = 520.0 nM 6.28
CHEMBL368022 EC50 = 550.0 nM 6.26
CHEMBL180545 EC50 = 560.0 nM 6.25
CHEMBL180304 EC50 = 570.0 nM 6.24
CHEMBL369348 EC50 = 570.0 nM 6.24
CHEMBL183134 EC50 = 630.0 nM 6.20
CHEMBL181277 EC50 = 640.0 nM 6.19
CHEMBL2113022 EC50 = 720.0 nM 6.14
CHEMBL183114 EC50 = 750.0 nM 6.12