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Assay Detail

CHEMBL1775437

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

Binding
Displacement of [125I]-2-iodomelatonin from human MT2 receptor expressed on CHO cells microscintillation counting
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Melatonin receptor type 1B (CHEMBL1946)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

1,6-Dihydro-2H-indeno[5,4-b]furan derivatives: design, synthesis, and pharmacological characterization of a novel class of highly potent MT₂-selective agonists.
Koike T, Hoashi Y, Takai T, Nakayama M, Yukuhiro N, Ishikawa T, Hirai K, Uchikawa O.
J Med Chem (2011) 54 : 3436 -3444
PubMed 21473625 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 10.43 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1774516 1 11.00
CHEMBL1774529 1 10.96
CHEMBL1774514 1 10.96
CHEMBL1774519 1 10.92
CHEMBL1774521 1 10.85
CHEMBL1774513 1 10.74
CHEMBL1774525 1 10.70
CHEMBL1774512 1 10.66
CHEMBL1774524 1 10.47
CHEMBL1774515 1 10.46
CHEMBL1774527 1 10.43
CHEMBL1774517 1 10.08
CHEMBL45 MELATONIN 4.0 1 9.68
CHEMBL1774528 1 9.47
CHEMBL1774530 1 9.11
CHEMBL1774518 1 -
CHEMBL1774520 1 -
CHEMBL1774522 1 -
CHEMBL1774523 1 -
CHEMBL1774526 1 -
CHEMBL1774531 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1774516 Ki = 0.01 nM 11.00
CHEMBL1774529 Ki = 0.011 nM 10.96
CHEMBL1774514 Ki = 0.011 nM 10.96
CHEMBL1774519 Ki = 0.012 nM 10.92
CHEMBL1774521 Ki = 0.014 nM 10.85
CHEMBL1774513 Ki = 0.018 nM 10.74
CHEMBL1774525 Ki = 0.02 nM 10.70
CHEMBL1774512 Ki = 0.022 nM 10.66
CHEMBL1774524 Ki = 0.034 nM 10.47
CHEMBL1774515 Ki = 0.035 nM 10.46
CHEMBL1774527 Ki = 0.037 nM 10.43
CHEMBL1774517 Ki = 0.084 nM 10.08
CHEMBL45 MELATONIN Ki = 0.21 nM 9.68
CHEMBL1774528 Ki = 0.34 nM 9.47
CHEMBL1774530 Ki = 0.77 nM 9.11
CHEMBL1774518 Ki = 0.0085 nM -
CHEMBL1774520 Ki = 0.0067 nM -
CHEMBL1774522 Ki = 0.0065 nM -
CHEMBL1774523 Ki = 0.0096 nM -
CHEMBL1774526 Ki = 0.009 nM -
CHEMBL1774531 Ki = 0.006 nM -