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Assay Detail

CHEMBL616345

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

Binding
Binding affinity towards 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand.
ChEMBL ↗
51
Total Activities
51
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

Three-dimensional quantitative structure-activity relationships of 5-HT receptor binding data for tetrahydropyridinylindole derivatives: a comparison of the Hansch and CoMFA methods.
Agarwal A, Pearson PP, Taylor EW, Li HB, Dahlgren T, Herslöf M, Yang Y, Lambert G, Nelson DL, Regan JW.
J Med Chem (1993) 36 : 4006 -4014
PubMed 8258822 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 51 6.92 8.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL283398 — — 1 8.28
CHEMBL27227 — — 1 7.96
CHEMBL18785 RU-24969 — 1 7.96
CHEMBL281432 — — 1 7.77
CHEMBL27643 — — 1 7.72
CHEMBL27719 — — 1 7.71
CHEMBL285777 — — 1 7.68
CHEMBL283416 — — 1 7.68
CHEMBL287576 — — 1 7.64
CHEMBL281434 — — 1 7.64
CHEMBL417470 — — 1 7.60
CHEMBL26900 — — 1 7.60
CHEMBL26311 — — 1 7.44
CHEMBL287097 — — 1 7.43
CHEMBL283899 — — 1 7.26
CHEMBL284107 — — 1 7.26
CHEMBL26836 — — 1 7.21
CHEMBL283257 — — 1 7.19
CHEMBL27025 — — 1 7.19
CHEMBL26972 — — 1 7.16
CHEMBL282799 — — 1 7.13
CHEMBL26322 — — 1 7.11
CHEMBL27998 — — 1 7.09
CHEMBL340175 — — 1 7.06
CHEMBL28105 — — 1 6.98
CHEMBL283397 — — 1 6.96
CHEMBL287441 — — 1 6.90
CHEMBL128544 — — 1 6.86
CHEMBL442534 — — 1 6.84
CHEMBL26655 — — 1 6.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL283398 — Ki = 5.297 nM 8.28
CHEMBL27227 — Ki = 10.96 nM 7.96
CHEMBL18785 RU-24969 Ki = 10.96 nM 7.96
CHEMBL281432 — Ki = 16.98 nM 7.77
CHEMBL27643 — Ki = 19.01 nM 7.72
CHEMBL27719 — Ki = 19.41 nM 7.71
CHEMBL285777 — Ki = 21.09 nM 7.68
CHEMBL283416 — Ki = 21.09 nM 7.68
CHEMBL287576 — Ki = 23.01 nM 7.64
CHEMBL281434 — Ki = 23.01 nM 7.64
CHEMBL417470 — Ki = 25.12 nM 7.60
CHEMBL26900 — Ki = 25.12 nM 7.60
CHEMBL26311 — Ki = 36.14 nM 7.44
CHEMBL287097 — Ki = 36.98 nM 7.43
CHEMBL284107 — Ki = 54.95 nM 7.26
CHEMBL283899 — Ki = 54.95 nM 7.26
CHEMBL26836 — Ki = 61.66 nM 7.21
CHEMBL283257 — Ki = 64.57 nM 7.19
CHEMBL27025 — Ki = 64.57 nM 7.19
CHEMBL26972 — Ki = 69.02 nM 7.16
CHEMBL282799 — Ki = 74.13 nM 7.13
CHEMBL26322 — Ki = 77.62 nM 7.11
CHEMBL27998 — Ki = 81.28 nM 7.09
CHEMBL340175 — Ki = 87.9 nM 7.06
CHEMBL28105 — Ki = 104.71 nM 6.98
CHEMBL283397 — Ki = 110.92 nM 6.96
CHEMBL287441 — Ki = 125.89 nM 6.90
CHEMBL128544 — Ki = 138.04 nM 6.86
CHEMBL442534 — Ki = 145.88 nM 6.84
CHEMBL26655 — Ki = 145.88 nM 6.84
CHEMBL128288 — Ki = 164.82 nM 6.78
CHEMBL286264 — Ki = 187.07 nM 6.73
CHEMBL287655 — Ki = 187.93 nM 6.73
CHEMBL283185 — Ki = 189.23 nM 6.72
CHEMBL27811 — Ki = 189.23 nM 6.72
CHEMBL539159 — Ki = 199.99 nM 6.70
CHEMBL280779 — Ki = 220.8 nM 6.66
CHEMBL281716 — Ki = 302.69 nM 6.52
CHEMBL284447 — Ki = 345.14 nM 6.46
CHEMBL25812 — Ki = 363.08 nM 6.44
CHEMBL26868 — Ki = 376.7 nM 6.42
CHEMBL131203 — Ki = 383.71 nM 6.42
CHEMBL341485 — Ki = 512.86 nM 6.29
CHEMBL337381 — Ki = 549.54 nM 6.26
CHEMBL26921 — Ki = 555.9 nM 6.25
CHEMBL26980 — Ki = 691.83 nM 6.16
CHEMBL285157 — Ki = 922.57 nM 6.04
CHEMBL26850 — Ki = 1786.49 nM 5.75
CHEMBL436568 — Ki = 2344.23 nM 5.63
CHEMBL130159 — Ki = 5533.5 nM 5.26