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Assay Detail

CHEMBL4358949

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

Binding
Displacement of [3H]2-BFI from I2IR in human brain frontal cortex incubated for 45 mins by liquid scintillation spectrometry
ChEMBL ↗
42
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Brain
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

Publication

Bicyclic α-Iminophosphonates as High Affinity Imidazoline I2 Receptor Ligands for Alzheimer's Disease.
Abás S, Rodríguez-Arévalo S, Bagán A, Griñán-Ferré C, Vasilopoulou F, Brocos-Mosquera I, Muguruza C, Pérez B, Molins E, Luque FJ, Pérez-Lozano P, de Jonghe S, Daelemans D, Naesens L, Brea J, Loza MI, Hernández-Hernández E, García-Sevilla JA, García-Fuster MJ, Radan M, Djikic T, Nikolic K, Pallàs M, Callado LF, Escolano C.
J Med Chem (2020) 63 : 3610 -3633
PubMed 32150414 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 42 6.99 10.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4482861 — — 1 10.28
CHEMBL4535472 — — 1 9.74
CHEMBL4450506 — — 2 8.56
CHEMBL4587519 — — 1 8.37
CHEMBL4459090 — — 1 7.97
CHEMBL4527478 — — 1 7.96
CHEMBL4590209 — — 1 7.90
CHEMBL4543019 — — 1 7.87
CHEMBL4546903 — — 1 7.73
CHEMBL4465834 — — 1 7.55
CHEMBL4554450 — — 1 7.35
CHEMBL4445396 — — 1 7.01
CHEMBL4533687 — — 1 6.96
CHEMBL4438801 — — 1 6.81
CHEMBL4467833 — — 1 6.79
CHEMBL4534152 — — 1 6.65
CHEMBL4469237 — — 1 6.59
CHEMBL4434967 — — 1 6.35
CHEMBL4456882 — — 1 5.81
CHEMBL4483022 — — 1 5.74
CHEMBL4461393 — — 1 5.44
CHEMBL4568994 — — 1 5.35
CHEMBL4438158 — — 1 5.26
CHEMBL4536304 — — 1 5.11
CHEMBL4528557 — — 1 5.09
CHEMBL4564836 — — 1 4.02
CHEMBL4454147 — — 1 -
CHEMBL4584406 — — 1 -
CHEMBL4439953 — — 1 -
CHEMBL4587003 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4482861 — Ki = 0.05248 nM 10.28
CHEMBL4535472 — Ki = 0.182 nM 9.74
CHEMBL4450506 — Ki = 2.754 nM 8.56
CHEMBL4450506 — Ki = 2.8 nM 8.55
CHEMBL4587519 — Ki = 4.266 nM 8.37
CHEMBL4459090 — Ki = 10.72 nM 7.97
CHEMBL4527478 — Ki = 10.96 nM 7.96
CHEMBL4590209 — Ki = 12.59 nM 7.90
CHEMBL4543019 — Ki = 13.49 nM 7.87
CHEMBL4546903 — Ki = 18.62 nM 7.73
CHEMBL4465834 — Ki = 28.18 nM 7.55
CHEMBL4554450 — Ki = 44.67 nM 7.35
CHEMBL4445396 — Ki = 97.72 nM 7.01
CHEMBL4533687 — Ki = 109.65 nM 6.96
CHEMBL4438801 — Ki = 154.88 nM 6.81
CHEMBL4467833 — Ki = 162.18 nM 6.79
CHEMBL4534152 — Ki = 223.87 nM 6.65
CHEMBL4469237 — Ki = 257.04 nM 6.59
CHEMBL4434967 — Ki = 446.68 nM 6.35
CHEMBL4456882 — Ki = 1548.82 nM 5.81
CHEMBL4483022 — Ki = 1819.7 nM 5.74
CHEMBL4461393 — Ki = 3630.78 nM 5.44
CHEMBL4568994 — Ki = 4466.84 nM 5.35
CHEMBL4438158 — Ki = 5495.41 nM 5.26
CHEMBL4536304 — Ki = 7762.47 nM 5.11
CHEMBL4528557 — Ki = 8128.31 nM 5.09
CHEMBL4564836 — Ki = 95499.26 nM 4.02
CHEMBL4593280 — Ki > 1000000.0 nM -
CHEMBL4443672 — Ki > 1000000.0 nM -
CHEMBL4513714 — Ki > 1000000.0 nM -
CHEMBL4459403 — Ki > 1000000.0 nM -
CHEMBL4543551 — Ki > 1000000.0 nM -
CHEMBL4577534 — Ki > 1000000.0 nM -
CHEMBL4475933 — Ki > 1000000.0 nM -
CHEMBL4534577 — Ki > 1000000.0 nM -
CHEMBL4476557 — Ki > 1000000.0 nM -
CHEMBL4531381 — Ki = 776247.12 nM -
CHEMBL4553853 — Ki = 144543.98 nM -
CHEMBL4587003 — Ki > 1000000.0 nM -
CHEMBL4439953 — Ki > 1000000.0 nM -
CHEMBL4584406 — Ki = 407380.28 nM -
CHEMBL4454147 — Ki > 1000000.0 nM -