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Assay Detail

CHEMBL616154

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

Binding
Binding affinity for rat cortex 5-hydroxytryptamine 1A receptor, by displacement of 0.2 nM [3H]8-OH-DPAT radioligand
71
Total Activities
71
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design and synthesis of a series of 6-substituted-2-pyridinylmethylamine derivatives as novel, high-affinity, selective agonists at 5-HT1A receptors.
Vacher B, Bonnaud B, Funes P, Jubault N, Koek W, Assié MB, Cosi C.
J Med Chem (1998) 41 : 5070 -5083
PubMed 9836623 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 71 7.80 9.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL46467 1 9.46
CHEMBL298260 1 9.43
CHEMBL45101 1 9.27
CHEMBL147119 1 9.20
CHEMBL42294 1 9.14
CHEMBL297138 1 9.03
CHEMBL348191 1 8.92
CHEMBL42618 1 8.86
CHEMBL42994 1 8.85
CHEMBL56 8-OH-DPAT 1 8.85
CHEMBL357773 1 8.85
CHEMBL147922 1 8.81
CHEMBL146669 1 8.80
CHEMBL295025 1 8.78
CHEMBL44904 1 8.76
CHEMBL149648 1 8.64
CHEMBL359444 1 8.59
CHEMBL280516 1 8.57
CHEMBL342754 1 8.50
CHEMBL145863 1 8.46
CHEMBL146868 1 8.46
CHEMBL262431 1 8.45
CHEMBL147341 1 8.45
CHEMBL147172 1 8.39
CHEMBL149302 1 8.37
CHEMBL146297 1 8.34
CHEMBL414623 1 8.22
CHEMBL358258 1 8.13
CHEMBL146589 1 8.13
CHEMBL146514 1 8.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL46467 Ki = 0.3467 nM 9.46
CHEMBL298260 Ki = 0.3715 nM 9.43
CHEMBL45101 Ki = 0.537 nM 9.27
CHEMBL147119 Ki = 0.631 nM 9.20
CHEMBL42294 Ki = 0.7244 nM 9.14
CHEMBL297138 Ki = 0.9333 nM 9.03
CHEMBL348191 Ki = 1.202 nM 8.92
CHEMBL42618 Ki = 1.38 nM 8.86
CHEMBL42994 Ki = 1.413 nM 8.85
CHEMBL56 8-OH-DPAT Ki = 1.413 nM 8.85
CHEMBL357773 Ki = 1.413 nM 8.85
CHEMBL147922 Ki = 1.549 nM 8.81
CHEMBL146669 Ki = 1.585 nM 8.80
CHEMBL295025 Ki = 1.66 nM 8.78
CHEMBL44904 Ki = 1.738 nM 8.76
CHEMBL149648 Ki = 2.291 nM 8.64
CHEMBL359444 Ki = 2.57 nM 8.59
CHEMBL280516 Ki = 2.692 nM 8.57
CHEMBL342754 Ki = 3.162 nM 8.50
CHEMBL145863 Ki = 3.467 nM 8.46
CHEMBL146868 Ki = 3.467 nM 8.46
CHEMBL262431 Ki = 3.548 nM 8.45
CHEMBL147341 Ki = 3.548 nM 8.45
CHEMBL147172 Ki = 4.074 nM 8.39
CHEMBL149302 Ki = 4.266 nM 8.37
CHEMBL146297 Ki = 4.571 nM 8.34
CHEMBL414623 Ki = 6.026 nM 8.22
CHEMBL358258 Ki = 7.413 nM 8.13
CHEMBL146589 Ki = 7.413 nM 8.13
CHEMBL146514 Ki = 8.913 nM 8.05
CHEMBL357655 Ki = 9.12 nM 8.04
CHEMBL357522 Ki = 9.12 nM 8.04
CHEMBL147479 Ki = 10.72 nM 7.97
CHEMBL149069 Ki = 11.75 nM 7.93
CHEMBL347060 Ki = 13.18 nM 7.88
CHEMBL358808 Ki = 13.49 nM 7.87
CHEMBL150184 Ki = 14.13 nM 7.85
CHEMBL149785 Ki = 14.79 nM 7.83
CHEMBL146394 Ki = 17.78 nM 7.75
CHEMBL147869 Ki = 17.78 nM 7.75
CHEMBL149120 Ki = 18.62 nM 7.73
CHEMBL46697 Ki = 26.3 nM 7.58
CHEMBL341628 Ki = 26.3 nM 7.58
CHEMBL356134 Ki = 27.54 nM 7.56
CHEMBL149148 Ki = 29.51 nM 7.53
CHEMBL146563 Ki = 33.11 nM 7.48
CHEMBL343671 Ki = 42.66 nM 7.37
CHEMBL148493 Ki = 46.77 nM 7.33
CHEMBL414443 Ki = 46.77 nM 7.33
CHEMBL146124 Ki = 48.98 nM 7.31