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Assay Detail

CHEMBL698412

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Functional
In vitro antagonistic activity against Histamine H3 receptor on Synaptosomes of rat cerebral cortex.
ChEMBL ↗
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Cerebral cortex
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Histamine H3 receptor (CHEMBL4124) ↗
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Novel carbamates as potent histamine H3 receptor antagonists with high in vitro and oral in vivo activity.
Stark H, Purand K, Ligneau X, Rouleau A, Arrang JM, Garbarg M, Schwartz JC, Schunack W.
J Med Chem (1996) 39 : 1157 -1163
PubMed 8676353 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 45 7.62 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL14690 CLOBENPROPIT — 1 9.22
CHEMBL260374 THIOPERAMIDE — 1 8.40
CHEMBL16231 — — 1 8.38
CHEMBL280249 (2-ferrocenyl)-carbamic acid 3-(1H-imidazol-4-yl)-propylester — 1 8.24
CHEMBL418172 — — 1 8.09
CHEMBL274262 — — 1 8.00
CHEMBL16348 — — 1 7.96
CHEMBL16874 — — 1 7.96
CHEMBL16056 — — 1 7.96
CHEMBL16592 — — 1 7.96
CHEMBL16496 — — 1 7.92
CHEMBL16654 — — 1 7.92
CHEMBL277537 — — 1 7.89
CHEMBL277149 — — 1 7.85
CHEMBL16142 — — 1 7.85
CHEMBL16957 — — 1 7.85
CHEMBL16565 — — 1 7.82
CHEMBL16338 — — 1 7.82
CHEMBL278025 — — 1 7.75
CHEMBL277989 — — 1 7.75
CHEMBL16108 — — 1 7.72
CHEMBL15883 — — 1 7.68
CHEMBL279617 — — 1 7.66
CHEMBL263070 — — 1 7.64
CHEMBL274989 — — 1 7.62
CHEMBL16373 — — 1 7.62
CHEMBL16639 — — 1 7.58
CHEMBL16640 — — 1 7.58
CHEMBL16109 — — 1 7.52
CHEMBL16407 — — 1 7.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL14690 CLOBENPROPIT Ki = 0.6 nM 9.22
CHEMBL260374 THIOPERAMIDE Ki = 4.0 nM 8.40
CHEMBL16231 — Ki = 4.2 nM 8.38
CHEMBL280249 (2-ferrocenyl)-carbamic acid 3-(1H-imidazol-4-yl)-propylester Ki = 5.8 nM 8.24
CHEMBL418172 — Ki = 8.1 nM 8.09
CHEMBL274262 — Ki = 10.0 nM 8.00
CHEMBL16348 — Ki = 11.0 nM 7.96
CHEMBL16874 — Ki = 11.0 nM 7.96
CHEMBL16056 — Ki = 11.0 nM 7.96
CHEMBL16592 — Ki = 11.0 nM 7.96
CHEMBL16496 — Ki = 12.0 nM 7.92
CHEMBL16654 — Ki = 12.0 nM 7.92
CHEMBL277537 — Ki = 13.0 nM 7.89
CHEMBL16957 — Ki = 14.0 nM 7.85
CHEMBL16142 — Ki = 14.0 nM 7.85
CHEMBL277149 — Ki = 14.0 nM 7.85
CHEMBL16565 — Ki = 15.0 nM 7.82
CHEMBL16338 — Ki = 15.0 nM 7.82
CHEMBL278025 — Ki = 18.0 nM 7.75
CHEMBL277989 — Ki = 18.0 nM 7.75
CHEMBL16108 — Ki = 19.0 nM 7.72
CHEMBL15883 — Ki = 21.0 nM 7.68
CHEMBL279617 — Ki = 22.0 nM 7.66
CHEMBL263070 — Ki = 23.0 nM 7.64
CHEMBL274989 — Ki = 24.0 nM 7.62
CHEMBL16373 — Ki = 24.0 nM 7.62
CHEMBL16639 — Ki = 26.0 nM 7.58
CHEMBL16640 — Ki = 26.0 nM 7.58
CHEMBL16109 — Ki = 30.0 nM 7.52
CHEMBL16407 — Ki = 32.0 nM 7.50
CHEMBL16319 — Ki = 34.0 nM 7.47
CHEMBL16331 — Ki = 42.0 nM 7.38
CHEMBL16876 — Ki = 49.0 nM 7.31
CHEMBL415989 — Ki = 50.0 nM 7.30
CHEMBL16524 — Ki = 52.0 nM 7.28
CHEMBL15830 — Ki = 56.0 nM 7.25
CHEMBL16401 — Ki = 64.0 nM 7.19
CHEMBL273549 — Ki = 69.0 nM 7.16
CHEMBL16593 — Ki = 69.0 nM 7.16
CHEMBL16682 — Ki = 95.0 nM 7.02
CHEMBL280001 — Ki = 95.0 nM 7.02
CHEMBL16274 — Ki = 114.0 nM 6.94
CHEMBL263071 — Ki = 165.0 nM 6.78
CHEMBL15842 — Ki = 355.0 nM 6.45
CHEMBL277285 — Ki = 541.0 nM 6.27