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Assay Detail

CHEMBL616346

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

Binding
Binding affinity towards 5-hydroxytryptamine 1A receptor in rat cortex using [3H]8-OH-DPAT as a radioligand
ChEMBL ↗
48
Total Activities
48
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

Novel derivatives of 2-pyridinemethylamine as selective, potent, and orally active agonists at 5-HT1A receptors.
Vacher B, Bonnaud B, Funes P, Jubault N, Koek W, Assié MB, Cosi C, Kleven M.
J Med Chem (1999) 42 : 1648 -1660
PubMed 10229633 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 48 9.00 10.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL45422 — — 1 10.12
CHEMBL42766 — — 1 10.01
CHEMBL360319 — — 1 9.92
CHEMBL46984 — — 1 9.83
CHEMBL288992 — — 1 9.73
CHEMBL45423 — — 1 9.70
CHEMBL45334 — — 1 9.69
CHEMBL44118 — — 1 9.67
CHEMBL46971 — — 1 9.61
CHEMBL295662 — — 1 9.57
CHEMBL42393 — — 1 9.55
CHEMBL46582 — — 1 9.52
CHEMBL45336 — — 1 9.50
CHEMBL46467 — — 1 9.46
CHEMBL298260 — — 1 9.43
CHEMBL42042 — — 1 9.35
CHEMBL46539 — — 1 9.34
CHEMBL46379 — — 1 9.33
CHEMBL44659 — — 1 9.33
CHEMBL44159 — — 1 9.31
CHEMBL45101 — — 1 9.27
CHEMBL296289 — — 1 9.25
CHEMBL47013 — — 1 9.24
CHEMBL42294 — — 1 9.14
CHEMBL46512 — — 1 9.10
CHEMBL45305 BEFIRADOL 2.0 1 9.07
CHEMBL297138 — — 1 9.03
CHEMBL43146 — — 1 8.98
CHEMBL3144354 — — 1 8.94
CHEMBL288244 — — 1 8.91

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL45422 — Ki = 0.07586 nM 10.12
CHEMBL42766 — Ki = 0.09772 nM 10.01
CHEMBL360319 — Ki = 0.1202 nM 9.92
CHEMBL46984 — Ki = 0.1479 nM 9.83
CHEMBL288992 — Ki = 0.1862 nM 9.73
CHEMBL45423 — Ki = 0.1995 nM 9.70
CHEMBL45334 — Ki = 0.2042 nM 9.69
CHEMBL44118 — Ki = 0.2138 nM 9.67
CHEMBL46971 — Ki = 0.2455 nM 9.61
CHEMBL295662 — Ki = 0.2692 nM 9.57
CHEMBL42393 — Ki = 0.2818 nM 9.55
CHEMBL46582 — Ki = 0.302 nM 9.52
CHEMBL45336 — Ki = 0.3162 nM 9.50
CHEMBL46467 — Ki = 0.3467 nM 9.46
CHEMBL298260 — Ki = 0.3715 nM 9.43
CHEMBL42042 — Ki = 0.4467 nM 9.35
CHEMBL46539 — Ki = 0.4571 nM 9.34
CHEMBL46379 — Ki = 0.4677 nM 9.33
CHEMBL44659 — Ki = 0.4677 nM 9.33
CHEMBL44159 — Ki = 0.4898 nM 9.31
CHEMBL45101 — Ki = 0.537 nM 9.27
CHEMBL296289 — Ki = 0.5623 nM 9.25
CHEMBL47013 — Ki = 0.5754 nM 9.24
CHEMBL42294 — Ki = 0.7244 nM 9.14
CHEMBL46512 — Ki = 0.7943 nM 9.10
CHEMBL45305 BEFIRADOL Ki = 0.8511 nM 9.07
CHEMBL297138 — Ki = 0.9333 nM 9.03
CHEMBL43146 — Ki = 1.047 nM 8.98
CHEMBL3144354 — Ki = 1.148 nM 8.94
CHEMBL288244 — Ki = 1.23 nM 8.91
CHEMBL42618 — Ki = 1.38 nM 8.86
CHEMBL45048 — Ki = 1.38 nM 8.86
CHEMBL42994 — Ki = 1.413 nM 8.85
CHEMBL44841 — Ki = 1.622 nM 8.79
CHEMBL295025 — Ki = 1.66 nM 8.78
CHEMBL440854 — Ki = 1.698 nM 8.77
CHEMBL44904 — Ki = 1.738 nM 8.76
CHEMBL42545 — Ki = 2.188 nM 8.66
CHEMBL46930 — Ki = 5.129 nM 8.29
CHEMBL43097 — Ki = 6.026 nM 8.22
CHEMBL297208 — Ki = 6.918 nM 8.16
CHEMBL431332 — Ki = 8.913 nM 8.05
CHEMBL45094 — Ki = 9.12 nM 8.04
CHEMBL42832 — Ki = 15.14 nM 7.82
CHEMBL46697 — Ki = 26.3 nM 7.58
CHEMBL44481 — Ki = 30.2 nM 7.52
CHEMBL432498 — Ki = 35.48 nM 7.45
CHEMBL45205 — Ki = 37.15 nM 7.43