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Assay Detail

CHEMBL712440

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

Binding
Competitive binding by the displacement of 2-[125I]- Iodomelatonin binding from melatonin receptors in chicken brain membranes
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Subcellular Membrane
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Melatonin receptor (CHEMBL2095154)
Type PROTEIN FAMILY
Organism Gallus gallus

Publication

Design and synthesis of new naphthalenic derivatives as ligands for 2-[125I]iodomelatonin binding sites.
Langlois M, Brémont B, Shen S, Poncet A, Andrieux J, Sicsic S, Serraz I, Mathé-Allainmat M, Renard P, Delagrange P.
J Med Chem (1995) 38 : 2050 -2060
PubMed 7783136 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 31 7.98 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL304203 1 10.30
CHEMBL291857 1 10.15
CHEMBL428882 1 10.00
CHEMBL61626 1 9.40
CHEMBL62992 1 9.27
CHEMBL10878 AGOMELATINE 4.0 1 9.27
CHEMBL294517 1 9.17
CHEMBL45 MELATONIN 4.0 1 9.17
CHEMBL64142 1 8.86
CHEMBL64471 1 8.57
CHEMBL305383 1 8.10
CHEMBL62574 1 7.76
CHEMBL59930 1 7.71
CHEMBL62306 1 7.38
CHEMBL63006 1 7.16
CHEMBL304685 1 6.72
CHEMBL53015 1 6.69
CHEMBL52801 1 6.67
CHEMBL291378 1 6.66
CHEMBL305075 1 6.62
CHEMBL53722 1 6.60
CHEMBL62495 1 6.49
CHEMBL304874 1 6.41
CHEMBL64699 1 6.38
CHEMBL66248 1 -
CHEMBL53721 1 -
CHEMBL63294 1 -
CHEMBL64651 1 -
CHEMBL65003 1 -
CHEMBL303598 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL304203 Ki = 0.05 nM 10.30
CHEMBL291857 Ki = 0.07 nM 10.15
CHEMBL428882 Ki = 0.1 nM 10.00
CHEMBL61626 Ki = 0.4 nM 9.40
CHEMBL62992 Ki = 0.54 nM 9.27
CHEMBL10878 AGOMELATINE Ki = 0.54 nM 9.27
CHEMBL294517 Ki = 0.68 nM 9.17
CHEMBL45 MELATONIN Ki = 0.67 nM 9.17
CHEMBL64142 Ki = 1.37 nM 8.86
CHEMBL64471 Ki = 2.68 nM 8.57
CHEMBL305383 Ki = 8.0 nM 8.10
CHEMBL62574 Ki = 17.5 nM 7.76
CHEMBL59930 Ki = 19.4 nM 7.71
CHEMBL62306 Ki = 42.0 nM 7.38
CHEMBL63006 Ki = 69.9 nM 7.16
CHEMBL304685 Ki = 192.0 nM 6.72
CHEMBL53015 Ki = 206.0 nM 6.69
CHEMBL52801 Ki = 213.0 nM 6.67
CHEMBL291378 Ki = 217.0 nM 6.66
CHEMBL305075 Ki = 237.0 nM 6.62
CHEMBL53722 Ki = 253.0 nM 6.60
CHEMBL62495 Ki = 321.0 nM 6.49
CHEMBL304874 Ki = 386.0 nM 6.41
CHEMBL64699 Ki = 421.0 nM 6.38
CHEMBL66248 Ki > 1000.0 nM -
CHEMBL53721 Ki > 1000.0 nM -
CHEMBL63294 Ki > 1000.0 nM -
CHEMBL64651 Ki > 1000.0 nM -
CHEMBL65003 Ki > 1000.0 nM -
CHEMBL303598 Ki > 1000.0 nM -
CHEMBL292242 Ki > 1000.0 nM -