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Assay Detail

CHEMBL1775434

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

Binding
Displacement of [125I]-2-iodomelatonin from human MT1 receptor expressed on CHO cells by 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 1A (CHEMBL1945)
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 9.42 10.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1774514 1 10.89
CHEMBL1774513 1 10.62
CHEMBL1774516 1 10.49
CHEMBL1774512 1 10.35
CHEMBL1774526 1 10.24
CHEMBL1774524 1 10.16
CHEMBL1774515 1 9.96
CHEMBL45 MELATONIN 4.0 1 9.62
CHEMBL1774520 1 9.06
CHEMBL1774517 1 8.96
CHEMBL1774525 1 8.96
CHEMBL1774531 1 8.89
CHEMBL1774530 1 8.85
CHEMBL1774518 1 8.57
CHEMBL1774527 1 8.52
CHEMBL1774519 1 8.04
CHEMBL1774529 1 7.89
CHEMBL1774521 1 -
CHEMBL1774522 1 -
CHEMBL1774523 1 -
CHEMBL1774528 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1774514 Ki = 0.013 nM 10.89
CHEMBL1774513 Ki = 0.024 nM 10.62
CHEMBL1774516 Ki = 0.032 nM 10.49
CHEMBL1774512 Ki = 0.045 nM 10.35
CHEMBL1774526 Ki = 0.057 nM 10.24
CHEMBL1774524 Ki = 0.069 nM 10.16
CHEMBL1774515 Ki = 0.11 nM 9.96
CHEMBL45 MELATONIN Ki = 0.24 nM 9.62
CHEMBL1774520 Ki = 0.88 nM 9.06
CHEMBL1774517 Ki = 1.1 nM 8.96
CHEMBL1774525 Ki = 1.1 nM 8.96
CHEMBL1774531 Ki = 1.3 nM 8.89
CHEMBL1774530 Ki = 1.4 nM 8.85
CHEMBL1774518 Ki = 2.7 nM 8.57
CHEMBL1774527 Ki = 3.0 nM 8.52
CHEMBL1774519 Ki = 9.2 nM 8.04
CHEMBL1774529 Ki = 13.0 nM 7.89
CHEMBL1774521 Ki = 0.0087 nM -
CHEMBL1774522 Ki = 0.0082 nM -
CHEMBL1774523 Ki = 0.0065 nM -
CHEMBL1774528 Ki > 100.0 nM -