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Assay Detail

CHEMBL4481483

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Binding
Displacement of [3H]NCS-382 from high-affinity GHB binding site of GABA(A) receptor in Sprague-Dawley rat cortical synaptic membranes by liquid scintillation counting
ChEMBL ↗
55
Total Activities
30
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

GABA-A receptor; anion channel (CHEMBL1907607) ↗
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

Discovery of 2-(Imidazo[1,2- b]pyridazin-2-yl)acetic Acid as a New Class of Ligands Selective for the γ-Hydroxybutyric Acid (GHB) High-Affinity Binding Sites.
Krall J, Bavo F, Falk-Petersen CB, Jensen CH, Nielsen JO, Tian Y, Anglani V, Kongstad KT, Piilgaard L, Nielsen B, Gloriam DE, Kehler J, Jensen AA, Harpsøe K, Wellendorph P, Frølund B.
J Med Chem (2019) 62 : 2798 -2813
PubMed 30763084 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 52 5.35 6.92
Inhibition 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1204604 — — 1 6.92
CHEMBL4578710 — — 2 6.77
CHEMBL4529526 — — 3 6.67
CHEMBL4571202 — — 2 6.65
CHEMBL4519194 — — 2 6.36
CHEMBL4593644 — — 2 6.33
CHEMBL4530576 — — 2 6.09
CHEMBL4581397 — — 2 5.67
CHEMBL1851667 — — 2 5.52
CHEMBL4588159 — — 2 5.39
CHEMBL1342 OXYBATE 4.0 1 5.37
CHEMBL4566181 — — 2 5.01
CHEMBL131516 — — 3 4.99
CHEMBL4586737 — — 2 4.90
CHEMBL4543048 — — 2 4.85
CHEMBL4515872 — — 2 4.83
CHEMBL4589563 — — 2 4.81
CHEMBL32503 GABAZINE — 1 4.80
CHEMBL4586160 — — 2 4.68
CHEMBL4570040 — — 2 4.53
CHEMBL4522479 — — 2 4.35
CHEMBL4538191 — — 2 4.14
CHEMBL133180 — — 2 4.01
CHEMBL4536994 — — 1 -
CHEMBL4553063 — — 1 -
CHEMBL4587203 — — 2 -
CHEMBL1091277 — — 1 -
CHEMBL1093534 — — 1 -
CHEMBL96 GAMMA-AMINOBUTYRIC ACID 1.0 1 -
CHEMBL4540258 — — 3 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1204604 — Ki = 120.0 nM 6.92
CHEMBL4578710 — Ki = 169.82 nM 6.77
CHEMBL4578710 — Ki = 190.0 nM 6.72
CHEMBL4529526 — Ki = 213.8 nM 6.67
CHEMBL4529526 — Ki = 220.0 nM 6.66
CHEMBL4571202 — Ki = 223.87 nM 6.65
CHEMBL4571202 — Ki = 230.0 nM 6.64
CHEMBL4519194 — Ki = 436.52 nM 6.36
CHEMBL4519194 — Ki = 440.0 nM 6.36
CHEMBL4593644 — Ki = 467.74 nM 6.33
CHEMBL4593644 — Ki = 510.0 nM 6.29
CHEMBL4530576 — Ki = 812.83 nM 6.09
CHEMBL4530576 — Ki = 830.0 nM 6.08
CHEMBL4581397 — Ki = 2137.96 nM 5.67
CHEMBL4581397 — Ki = 2200.0 nM 5.66
CHEMBL1851667 — Ki = 3019.95 nM 5.52
CHEMBL1851667 — Ki = 3100.0 nM 5.51
CHEMBL4588159 — Ki = 4073.8 nM 5.39
CHEMBL4588159 — Ki = 4200.0 nM 5.38
CHEMBL1342 OXYBATE Ki = 4300.0 nM 5.37
CHEMBL4566181 — Ki = 9772.37 nM 5.01
CHEMBL4566181 — Ki = 9900.0 nM 5.00
CHEMBL131516 — Ki = 10232.93 nM 4.99
CHEMBL131516 — Ki = 11000.0 nM 4.96
CHEMBL4586737 — Ki = 12589.25 nM 4.90
CHEMBL4586737 — Ki = 13000.0 nM 4.89
CHEMBL4543048 — Ki = 14000.0 nM 4.85
CHEMBL4543048 — Ki = 14454.4 nM 4.84
CHEMBL4515872 — Ki = 14791.08 nM 4.83
CHEMBL4515872 — Ki = 15000.0 nM 4.82
CHEMBL4589563 — Ki = 15488.17 nM 4.81
CHEMBL4589563 — Ki = 16000.0 nM 4.80
CHEMBL32503 GABAZINE Ki = 16000.0 nM 4.80
CHEMBL4586160 — Ki = 21000.0 nM 4.68
CHEMBL4586160 — Ki = 21877.62 nM 4.66
CHEMBL4570040 — Ki = 29512.09 nM 4.53
CHEMBL4570040 — Ki = 30000.0 nM 4.52
CHEMBL4522479 — Ki = 44668.36 nM 4.35
CHEMBL4522479 — Ki = 45000.0 nM 4.35
CHEMBL4538191 — Ki = 72443.6 nM 4.14
CHEMBL4538191 — Ki = 72000.0 nM 4.14
CHEMBL133180 — Ki = 97723.72 nM 4.01
CHEMBL133180 — Ki = 100000.0 nM 4.00
CHEMBL4536994 — Ki > 100000.0 nM -
CHEMBL4587203 — Ki = 389045.14 nM -
CHEMBL4540258 — Ki = 144543.98 nM -
CHEMBL4540258 — Ki = 146000.0 nM -
CHEMBL4553063 — Ki > 100000.0 nM -
CHEMBL4587203 — Ki = 427000.0 nM -
CHEMBL1091277 — Ki > 100000.0 nM -