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Assay Detail

CHEMBL4685402

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

Binding
Displacement of [3H]-LSD from recombinant human 5HT7 receptor expressed in CHOK1 cell membranes measured after 120 mins by microbeta counting method
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 7 (CHEMBL3155)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Multifunctional 6-fluoro-3-[3-(pyrrolidin-1-yl)propyl]-1,2-benzoxazoles targeting behavioral and psychological symptoms of dementia (BPSD).
Bucki A,Marcinkowska M,Śniecikowska J,Zagórska A,Jamrozik M,Pawłowski M,Głuch-Lutwin M,Siwek A,Jakubczyk M,Pytka K,Jastrzębska-Więsek M,Partyka A,Wesołowska A,Mierzejewski P,Kołaczkowski M
Eur J Med Chem (2020) 191 : 112149 -112149
PubMed 32105980 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 37 7.70 9.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL93240 METITEPINE 2.0 1 9.26
CHEMBL4775997 1 8.84
CHEMBL4750664 1 8.77
CHEMBL4754138 1 8.77
CHEMBL4784228 1 8.56
CHEMBL4758402 1 8.40
CHEMBL4795995 1 8.32
CHEMBL4793608 1 8.30
CHEMBL4763085 1 8.30
CHEMBL4747225 1 8.26
CHEMBL4759492 1 8.19
CHEMBL4764006 1 8.16
CHEMBL4753094 1 8.14
CHEMBL4776225 1 8.14
CHEMBL4742856 1 8.01
CHEMBL4779739 1 7.89
CHEMBL4782149 1 7.80
CHEMBL4764468 1 7.74
CHEMBL4754193 1 7.60
CHEMBL4750587 1 7.59
CHEMBL4741142 1 7.55
CHEMBL4747978 1 7.53
CHEMBL4796647 1 7.50
CHEMBL4785434 1 7.42
CHEMBL4749824 1 7.37
CHEMBL4778418 1 7.19
CHEMBL4784414 1 7.19
CHEMBL4762226 1 7.03
CHEMBL4744007 1 6.93
CHEMBL4764557 1 6.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL93240 METITEPINE Ki = 0.5495 nM 9.26
CHEMBL4775997 Ki = 1.445 nM 8.84
CHEMBL4754138 Ki = 1.698 nM 8.77
CHEMBL4750664 Ki = 1.698 nM 8.77
CHEMBL4784228 Ki = 2.754 nM 8.56
CHEMBL4758402 Ki = 3.981 nM 8.40
CHEMBL4795995 Ki = 4.786 nM 8.32
CHEMBL4793608 Ki = 5.012 nM 8.30
CHEMBL4763085 Ki = 5.012 nM 8.30
CHEMBL4747225 Ki = 5.495 nM 8.26
CHEMBL4759492 Ki = 6.457 nM 8.19
CHEMBL4764006 Ki = 6.918 nM 8.16
CHEMBL4753094 Ki = 7.244 nM 8.14
CHEMBL4776225 Ki = 7.244 nM 8.14
CHEMBL4742856 Ki = 9.772 nM 8.01
CHEMBL4779739 Ki = 12.88 nM 7.89
CHEMBL4782149 Ki = 15.85 nM 7.80
CHEMBL4764468 Ki = 18.2 nM 7.74
CHEMBL4754193 Ki = 25.12 nM 7.60
CHEMBL4750587 Ki = 25.7 nM 7.59
CHEMBL4741142 Ki = 28.18 nM 7.55
CHEMBL4747978 Ki = 29.51 nM 7.53
CHEMBL4796647 Ki = 31.62 nM 7.50
CHEMBL4785434 Ki = 38.02 nM 7.42
CHEMBL4749824 Ki = 42.66 nM 7.37
CHEMBL4778418 Ki = 64.57 nM 7.19
CHEMBL4784414 Ki = 64.57 nM 7.19
CHEMBL4762226 Ki = 93.33 nM 7.03
CHEMBL4744007 Ki = 117.49 nM 6.93
CHEMBL4764557 Ki = 120.23 nM 6.92
CHEMBL4760655 Ki = 125.89 nM 6.90
CHEMBL4780470 Ki = 131.83 nM 6.88
CHEMBL4763106 Ki = 169.82 nM 6.77
CHEMBL4790020 Ki = 218.78 nM 6.66
CHEMBL4748379 Ki = 229.09 nM 6.64
CHEMBL4751063 Ki = 229.09 nM 6.64
CHEMBL4748107 Ki = 245.47 nM 6.61