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Assay Detail

CHEMBL616201

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

Binding
In vitro binding affinity to rat hippocampal 5-hydroxytryptamine 1A receptor was determined using [3H]8-OH-DPAT as radioligand
ChEMBL ↗
54
Total Activities
54
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. 1. Discovery of a novel scaffold which embraces the D2 agonist pharmacophore. Structure-activity relationships of a series of 2-(aminomethyl)chromans.
Mewshaw RE, Kavanagh J, Stack G, Marquis KL, Shi X, Kagan MZ, Webb MB, Katz AH, Park A, Kang YH, Abou-Gharbia M, Scerni R, Wasik T, Cortes-Burgos L, Spangler T, Brennan JA, Piesla M, Mazandarani H, Cockett MI, Ochalski R, Coupet J, Andree TH.
J Med Chem (1997) 40 : 4235 -4256
PubMed 9435894 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 54 7.70 9.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL134677 — — 1 9.72
CHEMBL134930 — — 1 9.52
CHEMBL134489 — — 1 9.40
CHEMBL134605 — — 1 9.22
CHEMBL134707 — — 1 9.22
CHEMBL424087 — — 1 9.10
CHEMBL134281 — — 1 9.00
CHEMBL134448 — — 1 8.85
CHEMBL134663 — — 1 8.85
CHEMBL135201 — — 1 8.72
CHEMBL334616 — — 1 8.70
CHEMBL543426 — — 1 8.59
CHEMBL134678 — — 1 8.55
CHEMBL135222 — — 1 8.54
CHEMBL133833 — — 1 8.52
CHEMBL135495 — — 1 8.44
CHEMBL135242 — — 1 8.22
CHEMBL135752 — — 1 8.21
CHEMBL135183 — — 1 8.19
CHEMBL136635 — — 1 8.17
CHEMBL135546 — — 1 8.15
CHEMBL133367 — — 1 7.98
CHEMBL340267 — — 1 7.89
CHEMBL134807 — — 1 7.65
CHEMBL135137 — — 1 7.58
CHEMBL339190 — — 1 7.50
CHEMBL135044 — — 1 7.47
CHEMBL423335 — — 1 7.44
CHEMBL337724 — — 1 7.37
CHEMBL135873 — — 1 7.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL134677 — Ki = 0.19 nM 9.72
CHEMBL134930 — Ki = 0.3 nM 9.52
CHEMBL134489 — Ki = 0.4 nM 9.40
CHEMBL134605 — Ki = 0.6 nM 9.22
CHEMBL134707 — Ki = 0.6 nM 9.22
CHEMBL424087 — Ki = 0.8 nM 9.10
CHEMBL134281 — Ki = 1.0 nM 9.00
CHEMBL134448 — Ki = 1.4 nM 8.85
CHEMBL134663 — Ki = 1.4 nM 8.85
CHEMBL135201 — Ki = 1.9 nM 8.72
CHEMBL334616 — Ki = 2.0 nM 8.70
CHEMBL543426 — Ki = 2.6 nM 8.59
CHEMBL134678 — Ki = 2.8 nM 8.55
CHEMBL135222 — Ki = 2.9 nM 8.54
CHEMBL133833 — Ki = 3.0 nM 8.52
CHEMBL135495 — Ki = 3.6 nM 8.44
CHEMBL135242 — Ki = 6.0 nM 8.22
CHEMBL135752 — Ki = 6.2 nM 8.21
CHEMBL135183 — Ki = 6.5 nM 8.19
CHEMBL136635 — Ki = 6.8 nM 8.17
CHEMBL135546 — Ki = 7.0 nM 8.15
CHEMBL133367 — Ki = 10.5 nM 7.98
CHEMBL340267 — Ki = 13.0 nM 7.89
CHEMBL134807 — Ki = 22.5 nM 7.65
CHEMBL135137 — Ki = 26.5 nM 7.58
CHEMBL339190 — Ki = 31.5 nM 7.50
CHEMBL135044 — Ki = 33.5 nM 7.47
CHEMBL423335 — Ki = 36.0 nM 7.44
CHEMBL337724 — Ki = 42.5 nM 7.37
CHEMBL135873 — Ki = 43.5 nM 7.36
CHEMBL135211 — Ki = 46.0 nM 7.34
CHEMBL135864 — Ki = 50.0 nM 7.30
CHEMBL337696 — Ki = 52.0 nM 7.28
CHEMBL135395 — Ki = 52.0 nM 7.28
CHEMBL135297 — Ki = 56.0 nM 7.25
CHEMBL135285 — Ki = 57.5 nM 7.24
CHEMBL134655 — Ki = 59.5 nM 7.22
CHEMBL134843 — Ki = 67.0 nM 7.17
CHEMBL334406 — Ki = 71.5 nM 7.15
CHEMBL134725 — Ki = 77.0 nM 7.11
CHEMBL336856 — Ki = 86.0 nM 7.07
CHEMBL134808 — Ki = 110.0 nM 6.96
CHEMBL423890 — Ki = 156.0 nM 6.81
CHEMBL135636 — Ki = 177.0 nM 6.75
CHEMBL135291 — Ki = 192.0 nM 6.72
CHEMBL134582 — Ki = 208.0 nM 6.68
CHEMBL135357 — Ki = 214.0 nM 6.67
CHEMBL135116 — Ki = 268.0 nM 6.57
CHEMBL135269 — Ki = 308.0 nM 6.51
CHEMBL135011 — Ki = 330.0 nM 6.48