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Assay Detail

CHEMBL715564

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Binding
Binding affinity towards melatonin receptor, determined in chicken brain membranes using [2-125I]melatonin
70
Total Activities
62
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

Mapping the melatonin receptor. 5. Melatonin agonists and antagonists derived from tetrahydrocyclopent[b]indoles, tetrahydrocarbazoles and hexahydrocyclohept[b]indoles.
Davies DJ, Garratt PJ, Tocher DA, Vonhoff S, Davies J, Teh MT, Sugden D.
J Med Chem (1998) 41 : 451 -467
PubMed 9484496 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 70 7.00 9.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL53824 3 9.43
CHEMBL142343 1 9.42
CHEMBL45 MELATONIN 4.0 1 9.23
CHEMBL127826 1 8.84
CHEMBL143125 3 8.77
CHEMBL359451 1 8.70
CHEMBL141146 1 8.67
CHEMBL342723 3 8.19
CHEMBL143074 1 8.12
CHEMBL38520 1 8.08
CHEMBL335352 1 7.99
CHEMBL142567 1 7.79
CHEMBL141944 1 7.64
CHEMBL139873 1 7.62
CHEMBL143677 1 7.56
CHEMBL424297 1 7.52
CHEMBL140728 1 7.40
CHEMBL127827 3 7.40
CHEMBL287776 1 7.39
CHEMBL143547 1 7.35
CHEMBL345090 1 7.09
CHEMBL435080 1 7.08
CHEMBL417343 1 6.99
CHEMBL143524 1 6.89
CHEMBL141011 1 6.88
CHEMBL344521 1 6.85
CHEMBL288206 1 6.84
CHEMBL343878 1 6.84
CHEMBL358629 1 6.79
CHEMBL348238 1 6.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL53824 Ki = 0.372 nM 9.43
CHEMBL142343 Ki = 0.378 nM 9.42
CHEMBL45 MELATONIN Ki = 0.59 nM 9.23
CHEMBL53824 Ki = 0.97 nM 9.01
CHEMBL127826 Ki = 1.44 nM 8.84
CHEMBL143125 Ki = 1.7 nM 8.77
CHEMBL359451 Ki = 1.98 nM 8.70
CHEMBL141146 Ki = 2.12 nM 8.67
CHEMBL342723 Ki = 6.5 nM 8.19
CHEMBL342723 Ki = 7.0 nM 8.15
CHEMBL143074 Ki = 7.66 nM 8.12
CHEMBL38520 Ki = 8.3 nM 8.08
CHEMBL335352 Ki = 10.3 nM 7.99
CHEMBL143125 Ki = 16.0 nM 7.80
CHEMBL142567 Ki = 16.1 nM 7.79
CHEMBL141944 Ki = 23.0 nM 7.64
CHEMBL139873 Ki = 24.0 nM 7.62
CHEMBL143677 Ki = 27.5 nM 7.56
CHEMBL424297 Ki = 30.0 nM 7.52
CHEMBL127827 Ki = 40.0 nM 7.40
CHEMBL140728 Ki = 40.2 nM 7.40
CHEMBL287776 Ki = 41.0 nM 7.39
CHEMBL143547 Ki = 44.7 nM 7.35
CHEMBL53824 Ki = 48.4 nM 7.32
CHEMBL345090 Ki = 82.0 nM 7.09
CHEMBL435080 Ki = 84.0 nM 7.08
CHEMBL417343 Ki = 102.0 nM 6.99
CHEMBL143524 Ki = 129.0 nM 6.89
CHEMBL141011 Ki = 131.6 nM 6.88
CHEMBL344521 Ki = 141.7 nM 6.85
CHEMBL288206 Ki = 143.0 nM 6.84
CHEMBL343878 Ki = 144.8 nM 6.84
CHEMBL358629 Ki = 161.0 nM 6.79
CHEMBL348238 Ki = 187.2 nM 6.73
CHEMBL342723 Ki = 201.5 nM 6.70
CHEMBL127036 Ki = 204.0 nM 6.69
CHEMBL358401 Ki = 215.0 nM 6.67
CHEMBL41105 Ki = 219.0 nM 6.66
CHEMBL127827 Ki = 227.0 nM 6.64
CHEMBL142382 Ki = 239.0 nM 6.62
CHEMBL143125 Ki = 243.0 nM 6.61
CHEMBL343360 Ki = 272.0 nM 6.57
CHEMBL342335 Ki = 271.0 nM 6.57
CHEMBL358354 Ki = 424.0 nM 6.37
CHEMBL41148 Ki = 436.0 nM 6.36
CHEMBL143877 Ki = 459.0 nM 6.34
CHEMBL356536 Ki = 471.0 nM 6.33
CHEMBL140785 Ki = 516.0 nM 6.29
CHEMBL143543 Ki = 555.0 nM 6.26
CHEMBL290271 Ki = 560.0 nM 6.25