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Assay Detail

CHEMBL5535222

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Functional
Antagonist activity at human V1A receptor expressed in human 1321N1 cells assessed as Ca2+ mobilization incubated for 15 mins by FLIPR calcium 5 assay
ChEMBL ↗
70
Total Activities
70
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type 1321N1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Vasopressin V1a receptor (CHEMBL1889) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and Characterization of RGH-122, a Potent, Selective, and Orally Bioavailable V1a Receptor Antagonist.
Baska F, Bozó É, Szeleczky Z, Szántó G, Vukics K, Szakács Z, Domány-Kovács K, Kurkó D, Vass E, Thán M, Vastag M, Temesvári K, Lévai S, Halász AS, Szondiné Kordás K, Román V, Greiner I, Bata I.
J Med Chem (2024) 67 : 643 -673
PubMed 38165765 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 70 8.37 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5571796 — — 1 9.22
CHEMBL5575102 — — 1 9.22
CHEMBL5573173 — — 1 9.22
CHEMBL5574481 — — 1 9.10
CHEMBL5569717 — — 1 9.10
CHEMBL5571560 — — 1 9.10
CHEMBL5594994 — — 1 9.05
CHEMBL5571184 — — 1 9.05
CHEMBL5563054 — — 1 9.05
CHEMBL5565555 — — 1 9.05
CHEMBL4799793 — — 1 9.00
CHEMBL5549819 — — 1 8.96
CHEMBL5573091 — — 1 8.96
CHEMBL5070261 — — 1 8.96
CHEMBL5575281 — — 1 8.96
CHEMBL5572870 — — 1 8.92
CHEMBL5570415 — — 1 8.92
CHEMBL5074709 — — 1 8.92
CHEMBL5563095 — — 1 8.92
CHEMBL5572381 — — 1 8.92
CHEMBL5565605 — — 1 8.92
CHEMBL5570369 — — 1 8.89
CHEMBL5575561 — — 1 8.85
CHEMBL5575000 — — 1 8.85
CHEMBL5564659 — — 1 8.85
CHEMBL5573279 — — 1 8.74
CHEMBL5070075 — — 1 8.74
CHEMBL5595453 — — 1 8.74
CHEMBL5574628 — — 1 8.68
CHEMBL5572341 — — 1 8.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5571796 — IC50 = 0.6 nM 9.22
CHEMBL5575102 — IC50 = 0.6 nM 9.22
CHEMBL5573173 — IC50 = 0.6 nM 9.22
CHEMBL5574481 — IC50 = 0.8 nM 9.10
CHEMBL5569717 — IC50 = 0.8 nM 9.10
CHEMBL5571560 — IC50 = 0.8 nM 9.10
CHEMBL5565555 — IC50 = 0.9 nM 9.05
CHEMBL5563054 — IC50 = 0.9 nM 9.05
CHEMBL5571184 — IC50 = 0.9 nM 9.05
CHEMBL5594994 — IC50 = 0.9 nM 9.05
CHEMBL4799793 — IC50 = 1.0 nM 9.00
CHEMBL5070261 — IC50 = 1.1 nM 8.96
CHEMBL5575281 — IC50 = 1.1 nM 8.96
CHEMBL5573091 — IC50 = 1.1 nM 8.96
CHEMBL5549819 — IC50 = 1.1 nM 8.96
CHEMBL5572870 — IC50 = 1.2 nM 8.92
CHEMBL5565605 — IC50 = 1.2 nM 8.92
CHEMBL5572381 — IC50 = 1.2 nM 8.92
CHEMBL5563095 — IC50 = 1.2 nM 8.92
CHEMBL5074709 — IC50 = 1.2 nM 8.92
CHEMBL5570415 — IC50 = 1.2 nM 8.92
CHEMBL5570369 — IC50 = 1.3 nM 8.89
CHEMBL5575561 — IC50 = 1.4 nM 8.85
CHEMBL5575000 — IC50 = 1.4 nM 8.85
CHEMBL5564659 — IC50 = 1.4 nM 8.85
CHEMBL5573279 — IC50 = 1.8 nM 8.74
CHEMBL5595453 — IC50 = 1.8 nM 8.74
CHEMBL5070075 — IC50 = 1.8 nM 8.74
CHEMBL5574628 — IC50 = 2.1 nM 8.68
CHEMBL5572341 — IC50 = 2.1 nM 8.68
CHEMBL5571336 — IC50 = 2.2 nM 8.66
CHEMBL5575506 — IC50 = 2.3 nM 8.64
CHEMBL5572998 — IC50 = 2.3 nM 8.64
CHEMBL5568795 — IC50 = 2.3 nM 8.64
CHEMBL5573085 — IC50 = 2.4 nM 8.62
CHEMBL5594885 — IC50 = 2.5 nM 8.60
CHEMBL5571665 — IC50 = 2.5 nM 8.60
CHEMBL5592230 — IC50 = 2.8 nM 8.55
CHEMBL5563627 — IC50 = 2.9 nM 8.54
CHEMBL4297183 BALOVAPTAN IC50 = 3.0 nM 8.52
CHEMBL5584186 — IC50 = 4.0 nM 8.40
CHEMBL5574495 — IC50 = 4.5 nM 8.35
CHEMBL5570824 — IC50 = 4.7 nM 8.33
CHEMBL5542954 — IC50 = 4.9 nM 8.31
CHEMBL5583764 — IC50 = 5.4 nM 8.27
CHEMBL5593433 — IC50 = 5.4 nM 8.27
CHEMBL5569782 — IC50 = 6.3 nM 8.20
CHEMBL5563327 — IC50 = 6.8 nM 8.17
CHEMBL5573992 — IC50 = 6.9 nM 8.16
CHEMBL5579703 — IC50 = 7.0 nM 8.15