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Assay Detail

CHEMBL616879

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

Binding
Binding affinity towards human cloned 5-hydroxytryptamine 2A receptor of HEK293 cells by displacement of [3H]ketanserin
ChEMBL ↗
41
Total Activities
41
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 2A (CHEMBL224) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

1-[2-[(Heteroaryloxy)heteroaryl]carbamoyl]indolines: novel and selective 5-HT2C receptor inverse agonists with potential as antidepressant/anxiolytic agents.
Bromidge SM, Dabbs S, Davies S, Duckworth DM, Forbes IT, Jones GE, Jones J, King FD, Saunders DV, Blackburn TP, Holland V, Kennett GA, Lightowler S, Middlemiss DN, Riley GJ, Trail B, Wood MD.
Bioorg Med Chem Lett (2000) 10 : 1863 -1866
PubMed 10969986 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 41 6.58 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL55331 — — 1 8.10
CHEMBL55207 — — 1 7.80
CHEMBL55079 — — 1 7.20
CHEMBL299938 — — 1 7.10
CHEMBL294030 — — 1 7.00
CHEMBL301012 — — 1 6.90
CHEMBL55964 — — 1 6.90
CHEMBL53152 — — 1 6.90
CHEMBL292228 — — 1 6.80
CHEMBL291510 — — 1 6.80
CHEMBL14563 SB-242084 — 1 6.80
CHEMBL55472 — — 1 6.80
CHEMBL14460 SB-243213 — 1 6.80
CHEMBL59584 — — 1 6.80
CHEMBL55792 — — 1 6.70
CHEMBL56508 — — 1 6.60
CHEMBL54560 — — 1 6.60
CHEMBL301784 — — 1 6.60
CHEMBL299726 — — 1 6.50
CHEMBL58765 — — 1 6.40
CHEMBL299530 — — 1 6.30
CHEMBL55292 — — 1 6.30
CHEMBL52919 — — 1 6.30
CHEMBL53308 — — 1 6.20
CHEMBL299506 — — 1 6.20
CHEMBL14374 — — 1 6.10
CHEMBL56336 — — 1 6.10
CHEMBL53793 — — 1 6.10
CHEMBL433060 — — 1 5.80
CHEMBL52308 — — 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL55331 — Ki = 7.943 nM 8.10
CHEMBL55207 — Ki = 15.85 nM 7.80
CHEMBL55079 — Ki = 63.1 nM 7.20
CHEMBL299938 — Ki = 79.43 nM 7.10
CHEMBL294030 — Ki = 100.0 nM 7.00
CHEMBL301012 — Ki = 125.89 nM 6.90
CHEMBL55964 — Ki = 125.89 nM 6.90
CHEMBL53152 — Ki = 125.89 nM 6.90
CHEMBL55472 — Ki = 158.49 nM 6.80
CHEMBL291510 — Ki = 158.49 nM 6.80
CHEMBL14563 SB-242084 Ki = 158.49 nM 6.80
CHEMBL14460 SB-243213 Ki = 158.49 nM 6.80
CHEMBL59584 — Ki = 158.49 nM 6.80
CHEMBL292228 — Ki = 158.49 nM 6.80
CHEMBL55792 — Ki = 199.53 nM 6.70
CHEMBL56508 — Ki = 251.19 nM 6.60
CHEMBL301784 — Ki = 251.19 nM 6.60
CHEMBL54560 — Ki = 251.19 nM 6.60
CHEMBL299726 — Ki = 316.23 nM 6.50
CHEMBL58765 — Ki = 398.11 nM 6.40
CHEMBL299530 — Ki = 501.19 nM 6.30
CHEMBL52919 — Ki = 501.19 nM 6.30
CHEMBL55292 — Ki = 501.19 nM 6.30
CHEMBL53308 — Ki = 630.96 nM 6.20
CHEMBL299506 — Ki = 630.96 nM 6.20
CHEMBL14374 — Ki = 794.33 nM 6.10
CHEMBL56336 — Ki = 794.33 nM 6.10
CHEMBL53793 — Ki = 794.33 nM 6.10
CHEMBL433060 — Ki = 1584.89 nM 5.80
CHEMBL52308 — Ki = 1584.89 nM 5.80
CHEMBL54610 — Ki = 2511.89 nM 5.60
CHEMBL56050 — Ki = 3162.28 nM 5.50
CHEMBL54769 — Ki > 3981.07 nM -
CHEMBL53113 — Ki > 630.96 nM -
CHEMBL56232 — Ki > 10000.0 nM -
CHEMBL300232 — Ki > 10000.0 nM -
CHEMBL59097 — Ki > 10000.0 nM -
CHEMBL54775 — Ki > 1000.0 nM -
CHEMBL298696 — Ki > 10000.0 nM -
CHEMBL53053 — Ki > 6309.57 nM -
CHEMBL55958 — Ki > 10000.0 nM -