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Assay Detail

CHEMBL616203

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

Binding
In vitro binding affinity towards 5-hydroxytryptamine 1A receptor by the displacement of [3H]8-OH-DPAT radioligand in rat hippocampal homogenates
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Hippocampus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 1A (CHEMBL273)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

New generation dopaminergic agents. 6. Structure-activity relationship studies of a series of 4-(aminoethoxy)indole and 4-(aminoethoxy)indolone derivatives based on the newly discovered 3-hydroxyphenoxyethylamine D2 template.
Mewshaw RE, Webb MB, Marquis KL, McGaughey GB, Shi X, Wasik T, Scerni R, Brennan JA, Andree TH.
J Med Chem (1999) 42 : 2007 -2020
PubMed 10354409 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 41 7.06 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL59737 1 9.40
CHEMBL60185 1 9.40
CHEMBL61671 1 8.72
CHEMBL59501 1 8.10
CHEMBL303556 1 8.07
CHEMBL60265 1 7.92
CHEMBL300316 1 7.89
CHEMBL59750 1 7.77
CHEMBL292253 1 7.77
CHEMBL64553 1 7.65
CHEMBL418510 1 7.62
CHEMBL302436 1 7.60
CHEMBL291459 1 7.60
CHEMBL61665 1 7.42
CHEMBL64574 1 7.41
CHEMBL294538 1 7.39
CHEMBL64524 1 7.39
CHEMBL60840 1 7.29
CHEMBL60548 1 7.23
CHEMBL64466 1 7.08
CHEMBL62290 1 6.92
CHEMBL300571 1 6.81
CHEMBL64134 1 6.71
CHEMBL294204 1 6.66
CHEMBL60900 1 6.60
CHEMBL64238 1 6.56
CHEMBL59752 1 6.51
CHEMBL64798 1 6.47
CHEMBL63491 1 6.27
CHEMBL418681 1 6.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL59737 Ki = 0.4 nM 9.40
CHEMBL60185 Ki = 0.4 nM 9.40
CHEMBL61671 Ki = 1.9 nM 8.72
CHEMBL59501 Ki = 8.0 nM 8.10
CHEMBL303556 Ki = 8.5 nM 8.07
CHEMBL60265 Ki = 12.0 nM 7.92
CHEMBL300316 Ki = 13.0 nM 7.89
CHEMBL59750 Ki = 17.0 nM 7.77
CHEMBL292253 Ki = 17.0 nM 7.77
CHEMBL64553 Ki = 22.5 nM 7.65
CHEMBL418510 Ki = 24.0 nM 7.62
CHEMBL302436 Ki = 25.0 nM 7.60
CHEMBL291459 Ki = 25.0 nM 7.60
CHEMBL61665 Ki = 38.0 nM 7.42
CHEMBL64574 Ki = 39.0 nM 7.41
CHEMBL294538 Ki = 41.0 nM 7.39
CHEMBL64524 Ki = 41.0 nM 7.39
CHEMBL60840 Ki = 51.0 nM 7.29
CHEMBL60548 Ki = 59.0 nM 7.23
CHEMBL64466 Ki = 83.0 nM 7.08
CHEMBL62290 Ki = 121.0 nM 6.92
CHEMBL300571 Ki = 156.0 nM 6.81
CHEMBL64134 Ki = 193.0 nM 6.71
CHEMBL294204 Ki = 219.0 nM 6.66
CHEMBL60900 Ki = 253.0 nM 6.60
CHEMBL64238 Ki = 276.0 nM 6.56
CHEMBL59752 Ki = 306.0 nM 6.51
CHEMBL64798 Ki = 340.0 nM 6.47
CHEMBL63491 Ki = 535.0 nM 6.27
CHEMBL418681 Ki = 625.0 nM 6.20
CHEMBL416856 Ki = 664.0 nM 6.18
CHEMBL64345 Ki = 685.0 nM 6.16
CHEMBL305585 Ki = 1169.0 nM 5.93
CHEMBL64508 Ki = 1782.0 nM 5.75
CHEMBL302000 Ki = 1895.0 nM 5.72
CHEMBL435182 Ki = 2657.0 nM 5.58
CHEMBL434407 Ki = 6262.0 nM 5.20
CHEMBL59500 Ki = 6564.0 nM 5.18
CHEMBL59992 Ki - nM -
CHEMBL304894 Ki = - nM -
CHEMBL64509 Ki = - nM -