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Assay Detail

CHEMBL4351503

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

Binding
Displacement of [3H]Ro-15-1788 from human GABA alpha2/beta2/gamma2 receptor expressed in HEK cell membranes measured after 2 hrs by topcount method
ChEMBL ↗
50
Total Activities
50
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

Publication

Design and Identification of a Novel, Functionally Subtype Selective GABA<sub>A</sub> Positive Allosteric Modulator (PF-06372865).
Owen RM, Blakemore D, Cao L, Flanagan N, Fish R, Gibson KR, Gurrell R, Huh CW, Kammonen J, Mortimer-Cassen E, Nickolls SA, Omoto K, Owen D, Pike A, Pryde DC, Reynolds DS, Roeloffs R, Rose C, Stead C, Takeuchi M, Warmus JS, Watson C.
J Med Chem (2019) 62 : 5773 -5796
PubMed 30964988 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 50 7.53 9.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL200177 MK-0777 2.0 1 9.27
CHEMBL4303594 — — 1 9.09
CHEMBL204696 — — 1 8.67
CHEMBL4451323 — — 1 8.55
CHEMBL3647536 DARIGABAT 2.0 1 8.54
CHEMBL4545044 — — 1 8.18
CHEMBL4435952 — — 1 8.18
CHEMBL4446320 — — 1 8.17
CHEMBL4539265 — — 1 8.17
CHEMBL4443763 — — 1 8.14
CHEMBL3647565 — — 1 8.12
CHEMBL4558245 — — 1 8.06
CHEMBL4560422 — — 1 8.00
CHEMBL3647566 — — 1 7.94
CHEMBL3647539 — — 1 7.90
CHEMBL4470658 — — 1 7.89
CHEMBL4465623 — — 1 7.87
CHEMBL3647562 — — 1 7.75
CHEMBL3647568 — — 1 7.74
CHEMBL4587939 — — 1 7.74
CHEMBL4554992 — — 1 7.69
CHEMBL4438932 — — 1 7.66
CHEMBL3647559 — — 1 7.66
CHEMBL4457814 — — 1 7.64
CHEMBL4451804 — — 1 7.63
CHEMBL4439434 — — 1 7.63
CHEMBL4439739 — — 1 7.54
CHEMBL3647555 — — 1 7.53
CHEMBL4441213 — — 1 7.53
CHEMBL4471358 — — 1 7.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL200177 MK-0777 Ki = 0.54 nM 9.27
CHEMBL4303594 — Ki = 0.81 nM 9.09
CHEMBL204696 — Ki = 2.14 nM 8.67
CHEMBL4451323 — Ki = 2.8 nM 8.55
CHEMBL3647536 DARIGABAT Ki = 2.9 nM 8.54
CHEMBL4545044 — Ki = 6.6 nM 8.18
CHEMBL4435952 — Ki = 6.6 nM 8.18
CHEMBL4446320 — Ki = 6.7 nM 8.17
CHEMBL4539265 — Ki = 6.8 nM 8.17
CHEMBL4443763 — Ki = 7.3 nM 8.14
CHEMBL3647565 — Ki = 7.5 nM 8.12
CHEMBL4558245 — Ki = 8.8 nM 8.06
CHEMBL4560422 — Ki = 10.0 nM 8.00
CHEMBL3647566 — Ki = 11.6 nM 7.94
CHEMBL3647539 — Ki = 12.7 nM 7.90
CHEMBL4470658 — Ki = 12.8 nM 7.89
CHEMBL4465623 — Ki = 13.4 nM 7.87
CHEMBL3647562 — Ki = 17.7 nM 7.75
CHEMBL3647568 — Ki = 18.2 nM 7.74
CHEMBL4587939 — Ki = 18.4 nM 7.74
CHEMBL4554992 — Ki = 20.3 nM 7.69
CHEMBL4438932 — Ki = 21.7 nM 7.66
CHEMBL3647559 — Ki = 21.7 nM 7.66
CHEMBL4457814 — Ki = 22.8 nM 7.64
CHEMBL4439434 — Ki = 23.6 nM 7.63
CHEMBL4451804 — Ki = 23.2 nM 7.63
CHEMBL4439739 — Ki = 28.9 nM 7.54
CHEMBL3647555 — Ki = 29.7 nM 7.53
CHEMBL4441213 — Ki = 29.7 nM 7.53
CHEMBL4471358 — Ki = 30.6 nM 7.51
CHEMBL4461173 — Ki = 33.3 nM 7.48
CHEMBL4447071 — Ki = 33.3 nM 7.48
CHEMBL4445343 — Ki = 34.0 nM 7.47
CHEMBL4546051 — Ki = 40.6 nM 7.39
CHEMBL12 DIAZEPAM Ki = 48.3 nM 7.32
CHEMBL4584788 — Ki = 61.2 nM 7.21
CHEMBL4542431 — Ki = 71.6 nM 7.14
CHEMBL4456299 — Ki = 77.3 nM 7.11
CHEMBL4467015 — Ki = 81.3 nM 7.09
CHEMBL4461138 — Ki = 81.4 nM 7.09
CHEMBL4441464 — Ki = 119.5 nM 6.92
CHEMBL4473766 — Ki = 219.1 nM 6.66
CHEMBL4436710 — Ki = 274.6 nM 6.56
CHEMBL4464593 — Ki = 358.3 nM 6.45
CHEMBL4550007 — Ki = 367.3 nM 6.43
CHEMBL4455908 — Ki = 373.1 nM 6.43
CHEMBL4470660 — Ki = 655.9 nM 6.18
CHEMBL4543443 — Ki = 944.3 nM 6.03
CHEMBL4514448 — Ki = 961.6 nM 6.02
CHEMBL4575416 — Ki = 1141.9 nM 5.94