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Assay Detail

CHEMBL4049178

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

Binding
Displacement of [125I]-NDP-alpha-MSH from human MC1R LBD expressed in HEK293 cell membranes incubated for 16 to 23 hrs in dark by scintillation proximity assay
ChEMBL ↗
37
Total Activities
20
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Melanocyte-stimulating hormone receptor (CHEMBL3795) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of Novel Melanocortin Receptor Agonists Based on the Cyclic Peptide Framework of Sunflower Trypsin Inhibitor-1.
Durek T, Cromm PM, White AM, Schroeder CI, Kaas Q, Weidmann J, Ahmad Fuaad A, Cheneval O, Harvey PJ, Daly NL, Zhou Y, Dellsén A, Österlund T, Larsson N, Knerr L, Bauer U, Kessler H, Cai M, Hruby VJ, Plowright AT, Craik DJ.
J Med Chem (2018) 61 : 3674 -3684
PubMed 29605997 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 7.17 9.95
Inhibition 17 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL430239 MELATONAN — 1 9.95
CHEMBL4089162 — — 2 8.73
CHEMBL2070241 BREMELANOTIDE 4.0 1 8.72
CHEMBL4060381 — — 1 8.51
CHEMBL4101216 — — 2 8.41
CHEMBL4084765 — — 2 8.24
CHEMBL4067967 — — 2 8.17
CHEMBL4098785 — — 2 8.02
CHEMBL4074074 — — 2 7.52
CHEMBL4074479 — — 2 6.89
CHEMBL4102353 — — 2 6.66
CHEMBL4104465 — — 2 6.55
CHEMBL4073016 — — 2 6.47
CHEMBL4094606 — — 2 6.44
CHEMBL4063111 — — 2 6.31
CHEMBL4099889 — — 2 6.08
CHEMBL4064433 — — 2 5.98
CHEMBL4092141 — — 2 5.63
CHEMBL4080223 — — 2 5.33
CHEMBL4084386 — — 2 4.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL430239 MELATONAN Ki = 0.1122 nM 9.95
CHEMBL4089162 — Ki = 1.862 nM 8.73
CHEMBL2070241 BREMELANOTIDE Ki = 1.905 nM 8.72
CHEMBL4060381 — Ki = 3.09 nM 8.51
CHEMBL4101216 — Ki = 3.89 nM 8.41
CHEMBL4084765 — Ki = 5.754 nM 8.24
CHEMBL4067967 — Ki = 6.761 nM 8.17
CHEMBL4098785 — Ki = 9.55 nM 8.02
CHEMBL4074074 — Ki = 30.2 nM 7.52
CHEMBL4074479 — Ki = 128.82 nM 6.89
CHEMBL4102353 — Ki = 218.78 nM 6.66
CHEMBL4104465 — Ki = 281.84 nM 6.55
CHEMBL4073016 — Ki = 338.84 nM 6.47
CHEMBL4094606 — Ki = 363.08 nM 6.44
CHEMBL4063111 — Ki = 489.78 nM 6.31
CHEMBL4099889 — Ki = 831.76 nM 6.08
CHEMBL4064433 — Ki = 1047.13 nM 5.98
CHEMBL4092141 — Ki = 2344.23 nM 5.63
CHEMBL4080223 — Ki = 4677.35 nM 5.33
CHEMBL4084386 — Ki = 16982.44 nM 4.77
CHEMBL4074074 — Inhibition = 100.0 % -
CHEMBL4104465 — Inhibition = 100.0 % -
CHEMBL4080223 — Inhibition = 100.0 % -
CHEMBL4073016 — Inhibition = 100.0 % -
CHEMBL4099889 — Inhibition = 100.0 % -
CHEMBL4064433 — Inhibition = 100.0 % -
CHEMBL4092141 — Inhibition = 100.0 % -
CHEMBL4102353 — Inhibition = 100.0 % -
CHEMBL4084386 — Inhibition = 100.0 % -
CHEMBL4063111 — Inhibition = 100.0 % -
CHEMBL4084765 — Inhibition = 100.0 % -
CHEMBL4101216 — Inhibition = 100.0 % -
CHEMBL4074479 — Inhibition = 100.0 % -
CHEMBL4067967 — Inhibition = 100.0 % -
CHEMBL4089162 — Inhibition = 100.0 % -
CHEMBL4098785 — Inhibition = 100.0 % -
CHEMBL4094606 — Inhibition = 100.0 % -