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Assay Detail

CHEMBL904136

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

Binding
Displacement of [3H]flumazenil from bovine brain cortex GABAA/Bz receptor
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Novel 3-iodo-8-ethoxypyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide as promising lead for design of alpha5-inverse agonist useful tools for therapy of mnemonic damage.
Guerrini G, Ciciani G, Cambi G, Bruni F, Selleri S, Besnard F, Montali M, Martini C, Ghelardini C, Galeotti N, Costanzo A.
Bioorg Med Chem (2007) 15 : 2573 -2586
PubMed 17306981 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 31 7.50 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL228342 1 9.10
CHEMBL229145 1 8.77
CHEMBL229144 1 8.32
CHEMBL228288 1 8.27
CHEMBL390950 1 8.19
CHEMBL228290 1 8.12
CHEMBL12 DIAZEPAM 4.0 1 8.00
CHEMBL389391 1 7.92
CHEMBL229143 1 7.92
CHEMBL229198 1 7.87
CHEMBL229901 1 7.85
CHEMBL229142 1 7.85
CHEMBL229928 1 7.81
CHEMBL390165 1 7.80
CHEMBL388601 1 7.75
CHEMBL229900 1 7.64
CHEMBL228287 1 7.43
CHEMBL376329 1 7.43
CHEMBL228395 1 7.38
CHEMBL229848 1 7.27
CHEMBL443057 1 7.21
CHEMBL376123 1 7.14
CHEMBL376124 1 7.09
CHEMBL229847 1 6.92
CHEMBL229846 1 6.80
CHEMBL229845 1 6.71
CHEMBL229897 1 6.70
CHEMBL228291 1 6.63
CHEMBL229896 1 6.48
CHEMBL229133 1 6.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL228342 Ki = 0.8 nM 9.10
CHEMBL229145 Ki = 1.7 nM 8.77
CHEMBL229144 Ki = 4.8 nM 8.32
CHEMBL228288 Ki = 5.4 nM 8.27
CHEMBL390950 Ki = 6.5 nM 8.19
CHEMBL228290 Ki = 7.6 nM 8.12
CHEMBL12 DIAZEPAM Ki = 10.0 nM 8.00
CHEMBL389391 Ki = 12.0 nM 7.92
CHEMBL229143 Ki = 12.0 nM 7.92
CHEMBL229198 Ki = 13.5 nM 7.87
CHEMBL229901 Ki = 14.0 nM 7.85
CHEMBL229142 Ki = 14.0 nM 7.85
CHEMBL229928 Ki = 15.6 nM 7.81
CHEMBL390165 Ki = 15.8 nM 7.80
CHEMBL388601 Ki = 18.0 nM 7.75
CHEMBL229900 Ki = 22.8 nM 7.64
CHEMBL228287 Ki = 37.0 nM 7.43
CHEMBL376329 Ki = 36.9 nM 7.43
CHEMBL228395 Ki = 42.0 nM 7.38
CHEMBL229848 Ki = 53.2 nM 7.27
CHEMBL443057 Ki = 62.0 nM 7.21
CHEMBL376123 Ki = 73.0 nM 7.14
CHEMBL376124 Ki = 81.0 nM 7.09
CHEMBL229847 Ki = 120.0 nM 6.92
CHEMBL229846 Ki = 160.0 nM 6.80
CHEMBL229845 Ki = 196.0 nM 6.71
CHEMBL229897 Ki = 202.0 nM 6.70
CHEMBL228291 Ki = 233.0 nM 6.63
CHEMBL229896 Ki = 332.0 nM 6.48
CHEMBL229133 Ki = 374.0 nM 6.43
CHEMBL229196 Ki = 1700.0 nM 5.77