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Assay Detail

CHEMBL856174

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

Binding
Melatonin receptor type 1A binding affinity measured using 2-[125I]iodomelatonin on ovine pars tuberalis membrane homogenates.
ChEMBL ↗
141
Total Activities
141
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Ovis aries
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Melatonin receptor type 1A (CHEMBL1945) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pharmacophoric search and 3D-QSAR comparative molecular field analysis studies on agonists of melatonin sheep receptors.
Marot C, Chavatte P, Morin-Allory L, Viaud MC, Guillaumet G, Renard P, Lesieur D, Michel A.
J Med Chem (1998) 41 : 4453 -4465
PubMed 9804685 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 141 7.17 10.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL139855 — — 1 10.90
CHEMBL329263 — — 1 10.80
CHEMBL11356 — — 1 9.80
CHEMBL274358 — — 1 9.60
CHEMBL337764 — — 1 9.50
CHEMBL137998 — — 1 9.10
CHEMBL137878 — — 1 9.10
CHEMBL322762 — — 1 9.10
CHEMBL38728 — — 1 9.00
CHEMBL138321 — — 1 9.00
CHEMBL289233 IODOMELATONIN — 1 9.00
CHEMBL109235 — — 1 8.90
CHEMBL417151 — — 1 8.90
CHEMBL11404 — — 1 8.90
CHEMBL113441 — — 1 8.90
CHEMBL323332 — — 1 8.80
CHEMBL109086 — — 1 8.70
CHEMBL138766 — — 1 8.70
CHEMBL37771 — — 1 8.70
CHEMBL37703 — — 1 8.60
CHEMBL138817 — — 1 8.60
CHEMBL140549 — — 1 8.50
CHEMBL141115 — — 1 8.50
CHEMBL436006 — — 1 8.50
CHEMBL335116 — — 1 8.40
CHEMBL441664 — — 1 8.40
CHEMBL337580 — — 1 8.40
CHEMBL321612 — — 1 8.40
CHEMBL320253 — — 1 8.30
CHEMBL138440 — — 1 8.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL139855 — IC50 = 0.01259 nM 10.90
CHEMBL329263 — IC50 = 0.01585 nM 10.80
CHEMBL11356 — IC50 = 0.1585 nM 9.80
CHEMBL274358 — IC50 = 0.2512 nM 9.60
CHEMBL337764 — IC50 = 0.3162 nM 9.50
CHEMBL137998 — IC50 = 0.7943 nM 9.10
CHEMBL137878 — IC50 = 0.7943 nM 9.10
CHEMBL322762 — IC50 = 0.7943 nM 9.10
CHEMBL138321 — IC50 = 1.0 nM 9.00
CHEMBL289233 IODOMELATONIN IC50 = 1.0 nM 9.00
CHEMBL38728 — IC50 = 1.0 nM 9.00
CHEMBL417151 — IC50 = 1.259 nM 8.90
CHEMBL113441 — IC50 = 1.259 nM 8.90
CHEMBL11404 — IC50 = 1.259 nM 8.90
CHEMBL109235 — IC50 = 1.259 nM 8.90
CHEMBL323332 — IC50 = 1.585 nM 8.80
CHEMBL37771 — IC50 = 1.995 nM 8.70
CHEMBL109086 — IC50 = 1.995 nM 8.70
CHEMBL138766 — IC50 = 1.995 nM 8.70
CHEMBL138817 — IC50 = 2.512 nM 8.60
CHEMBL37703 — IC50 = 2.512 nM 8.60
CHEMBL140549 — IC50 = 3.162 nM 8.50
CHEMBL141115 — IC50 = 3.162 nM 8.50
CHEMBL436006 — IC50 = 3.162 nM 8.50
CHEMBL321612 — IC50 = 3.981 nM 8.40
CHEMBL441664 — IC50 = 3.981 nM 8.40
CHEMBL335116 — IC50 = 3.981 nM 8.40
CHEMBL337580 — IC50 = 3.981 nM 8.40
CHEMBL110980 — IC50 = 5.012 nM 8.30
CHEMBL138440 — IC50 = 5.012 nM 8.30
CHEMBL138752 — IC50 = 5.012 nM 8.30
CHEMBL320253 — IC50 = 5.012 nM 8.30
CHEMBL137910 — IC50 = 5.012 nM 8.30
CHEMBL139014 — IC50 = 6.31 nM 8.20
CHEMBL139410 — IC50 = 6.31 nM 8.20
CHEMBL111718 — IC50 = 6.31 nM 8.20
CHEMBL342655 — IC50 = 7.943 nM 8.10
CHEMBL342432 — IC50 = 7.943 nM 8.10
CHEMBL138549 — IC50 = 7.943 nM 8.10
CHEMBL344268 — IC50 = 7.943 nM 8.10
CHEMBL336010 — IC50 = 7.943 nM 8.10
CHEMBL138288 — IC50 = 10.0 nM 8.00
CHEMBL341761 — IC50 = 10.0 nM 8.00
CHEMBL11328 — IC50 = 10.0 nM 8.00
CHEMBL336225 — IC50 = 12.59 nM 7.90
CHEMBL342592 — IC50 = 12.59 nM 7.90
CHEMBL139516 — IC50 = 12.59 nM 7.90
CHEMBL139228 — IC50 = 12.59 nM 7.90
CHEMBL344880 — IC50 = 12.59 nM 7.90
CHEMBL138201 — IC50 = 15.85 nM 7.80