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Assay Detail

CHEMBL617752

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

Binding
Binding affinity towards cloned human 5-hydroxytryptamine 2C receptor expressed in HEK 293 cells using [3H]mesulergine as radioligand
ChEMBL ↗
56
Total Activities
56
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 2C (CHEMBL225) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel and selective 5-HT2C/2B receptor antagonists as potential anxiolytic agents: synthesis, quantitative structure-activity relationships, and molecular modeling of substituted 1-(3-pyridylcarbamoyl)indolines.
Bromidge SM, Dabbs S, Davies DT, Duckworth DM, Forbes IT, Ham P, Jones GE, King FD, Saunders DV, Starr S, Thewlis KM, Wyman PA, Blaney FE, Naylor CB, Bailey F, Blackburn TP, Holland V, Kennett GA, Riley GJ, Wood MD.
J Med Chem (1998) 41 : 1598 -1612
PubMed 9572885 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 56 7.67 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL41940 — — 1 8.70
CHEMBL288129 — — 1 8.70
CHEMBL276140 — — 1 8.60
CHEMBL417713 — — 1 8.60
CHEMBL41389 — — 1 8.50
CHEMBL43929 — — 1 8.50
CHEMBL296090 — — 1 8.50
CHEMBL289436 — — 1 8.50
CHEMBL43916 — — 1 8.40
CHEMBL42681 — — 1 8.40
CHEMBL44015 — — 1 8.40
CHEMBL43808 — — 1 8.30
CHEMBL42024 — — 1 8.20
CHEMBL296189 — — 1 8.20
CHEMBL41510 — — 1 8.20
CHEMBL41792 — — 1 8.20
CHEMBL265991 — — 1 8.20
CHEMBL42463 — — 1 8.10
CHEMBL297043 — — 1 8.10
CHEMBL44095 — — 1 8.00
CHEMBL14352 — — 1 8.00
CHEMBL416806 — — 1 7.90
CHEMBL42257 — — 1 7.90
CHEMBL297784 — — 1 7.90
CHEMBL40342 — — 1 7.80
CHEMBL42758 — — 1 7.80
CHEMBL290666 — — 1 7.70
CHEMBL43633 — — 1 7.70
CHEMBL297445 — — 1 7.70
CHEMBL296687 — — 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL41940 — Ki = 1.995 nM 8.70
CHEMBL288129 — Ki = 1.995 nM 8.70
CHEMBL417713 — Ki = 2.512 nM 8.60
CHEMBL276140 — Ki = 2.512 nM 8.60
CHEMBL41389 — Ki = 3.162 nM 8.50
CHEMBL43929 — Ki = 3.162 nM 8.50
CHEMBL296090 — Ki = 3.162 nM 8.50
CHEMBL289436 — Ki = 3.162 nM 8.50
CHEMBL43916 — Ki = 3.981 nM 8.40
CHEMBL42681 — Ki = 3.981 nM 8.40
CHEMBL44015 — Ki = 3.981 nM 8.40
CHEMBL43808 — Ki = 5.012 nM 8.30
CHEMBL41792 — Ki = 6.31 nM 8.20
CHEMBL296189 — Ki = 6.31 nM 8.20
CHEMBL42024 — Ki = 6.31 nM 8.20
CHEMBL41510 — Ki = 6.31 nM 8.20
CHEMBL265991 — Ki = 6.31 nM 8.20
CHEMBL42463 — Ki = 7.943 nM 8.10
CHEMBL297043 — Ki = 7.943 nM 8.10
CHEMBL44095 — Ki = 10.0 nM 8.00
CHEMBL14352 — Ki = 10.0 nM 8.00
CHEMBL416806 — Ki = 12.59 nM 7.90
CHEMBL42257 — Ki = 12.59 nM 7.90
CHEMBL297784 — Ki = 12.59 nM 7.90
CHEMBL42758 — Ki = 15.85 nM 7.80
CHEMBL40342 — Ki = 15.85 nM 7.80
CHEMBL290666 — Ki = 19.95 nM 7.70
CHEMBL43633 — Ki = 19.95 nM 7.70
CHEMBL297445 — Ki = 19.95 nM 7.70
CHEMBL296687 — Ki = 19.95 nM 7.70
CHEMBL289063 — Ki = 25.12 nM 7.60
CHEMBL296791 — Ki = 25.12 nM 7.60
CHEMBL44206 — Ki = 25.12 nM 7.60
CHEMBL443518 — Ki = 25.12 nM 7.60
CHEMBL42276 — Ki = 25.12 nM 7.60
CHEMBL40699 — Ki = 31.62 nM 7.50
CHEMBL42806 — Ki = 31.62 nM 7.50
CHEMBL40341 — Ki = 31.62 nM 7.50
CHEMBL38027 — Ki = 39.81 nM 7.40
CHEMBL44552 — Ki = 39.81 nM 7.40
CHEMBL288108 — Ki = 50.12 nM 7.30
CHEMBL38911 — Ki = 50.12 nM 7.30
CHEMBL43496 — Ki = 50.12 nM 7.30
CHEMBL295020 — Ki = 50.12 nM 7.30
CHEMBL431729 — Ki = 63.1 nM 7.20
CHEMBL290395 — Ki = 79.43 nM 7.10
CHEMBL40698 — Ki = 79.43 nM 7.10
CHEMBL296236 — Ki = 125.89 nM 6.90
CHEMBL40579 — Ki = 125.89 nM 6.90
CHEMBL41153 — Ki = 158.49 nM 6.80