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Assay Detail

CHEMBL1785092

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

Binding
Displacement of [3H]epibatidine from nAChR in rat cerebral cortex
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Cerebral cortex
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Polyethylene glycol-based homologated ligands for nicotinic acetylcholine receptors.
Scates BA, Lashbrook BL, Chastain BC, Tominaga K, Elliott BT, Theising NJ, Baker TA, Fitch RW.
Bioorg Med Chem (2008) 16 : 10295 -10300
PubMed 19006672 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 24 5.89 8.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL175428 1 8.51
CHEMBL1785039 1 8.33
CHEMBL1785041 1 8.12
CHEMBL1785042 1 7.82
CHEMBL1785040 1 7.82
CHEMBL1785043 1 7.52
CHEMBL1785044 1 7.40
CHEMBL1785045 1 7.20
CHEMBL1785032 1 6.17
CHEMBL1785033 1 5.52
CHEMBL1785001 ACETYLDIMETHYLPIPERAZINIUM IODIDE 1 5.44
CHEMBL1785034 1 5.09
CHEMBL1784994 1 4.85
CHEMBL1785038 1 4.72
CHEMBL1785036 1 4.58
CHEMBL1785000 1 4.52
CHEMBL1784996 1 4.50
CHEMBL1785037 1 4.42
CHEMBL1785035 1 4.32
CHEMBL1784995 1 4.27
CHEMBL1784993 ACETYLAMINOCHOLINE IODIDE 1 4.20
CHEMBL1784997 1 4.16
CHEMBL1784999 1 -
CHEMBL1784998 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL175428 Ki = 3.1 nM 8.51
CHEMBL1785039 Ki = 4.7 nM 8.33
CHEMBL1785041 Ki = 7.5 nM 8.12
CHEMBL1785042 Ki = 15.0 nM 7.82
CHEMBL1785040 Ki = 15.0 nM 7.82
CHEMBL1785043 Ki = 30.0 nM 7.52
CHEMBL1785044 Ki = 40.0 nM 7.40
CHEMBL1785045 Ki = 63.0 nM 7.20
CHEMBL1785032 Ki = 670.0 nM 6.17
CHEMBL1785033 Ki = 3000.0 nM 5.52
CHEMBL1785001 ACETYLDIMETHYLPIPERAZINIUM IODIDE Ki = 3600.0 nM 5.44
CHEMBL1785034 Ki = 8200.0 nM 5.09
CHEMBL1784994 Ki = 14000.0 nM 4.85
CHEMBL1785038 Ki = 19000.0 nM 4.72
CHEMBL1785036 Ki = 26000.0 nM 4.58
CHEMBL1785000 Ki = 30000.0 nM 4.52
CHEMBL1784996 Ki = 32000.0 nM 4.50
CHEMBL1785037 Ki = 38000.0 nM 4.42
CHEMBL1785035 Ki = 48000.0 nM 4.32
CHEMBL1784995 Ki = 54000.0 nM 4.27
CHEMBL1784993 ACETYLAMINOCHOLINE IODIDE Ki = 63000.0 nM 4.20
CHEMBL1784997 Ki = 70000.0 nM 4.16
CHEMBL1784999 Ki = 190000.0 nM -
CHEMBL1784998 Ki = 150000.0 nM -