ChEMBL ligand: CHEMBL2364638 (MK-1602, Ubrelvy, Ubrogepant, Ubrogepant anhydrous)
RAMP1/calcitonin receptor-like receptor/Calcitonin-gene-related peptide receptor, CALCRL/RAMP1 in Human [ChEMBL: CHEMBL2107838] [GtoPdb: 51, 47] [UniProtKB: O60894, Q16602] There should be some charts here, you may need to enable JavaScript!
calcitonin receptor-like receptor/Calcitonin gene-related peptide type 1 receptor in Human [ChEMBL: CHEMBL3798] [GtoPdb: 47] [UniProtKB: Q16602] There should be some charts here, you may need to enable JavaScript!
CGRP receptor in Human [GtoPdb: 48] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
RAMP1/calcitonin receptor-like receptor/Calcitonin-gene-related peptide receptor, CALCRL/RAMP1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2107838] [GtoPdb: 51, 47] [UniProtKB: O60894, Q16602]
ChEMBL	Displacement of [125I]hCGRP from human recombinant CGRP receptor expressed in HEK293 cell membranes incubated for 3 hrs by scintillation counting method	B	10.17	pKi	0.07	nM	Ki	US-8481556-B2. Piperidinone carboxamide azaindane CGRP receptor antagonists (2013)
ChEMBL	Antagonist activity at human CLR/RAMP1	B	10.17	pKi	0.07	nM	Ki	J Med Chem (2020) 63: 6600-6623 [PMID:32058712]
calcitonin receptor-like receptor/Calcitonin gene-related peptide type 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3798] [GtoPdb: 47] [UniProtKB: Q16602]
ChEMBL	Receptor Functional Assay: Cells were resuspended in DMEM/F12 (Hyclone) supplemented with 1 g/L BSA and 300 μM isobutyl-methylxanthine. Cells were then plated in a 384-well plate (Proxiplate Plus 384; 509052761; Perkin-Elmer) at a density of 2,000 cells/well and incubated with antagonist for 30 min at 37° C. Human α-CGRP was then added to the cells at a final concentration of 1.2 nM and incubated an additional 20 min at 37° C. Following agonist stimulation, the cells were processed for cAMP determination using the two-step procedure according to the manufacturer's recommended protocol (HTRF cAMP dynamic 2 assay kit; 62AM4PEC; Cisbio). Raw data were transformed into concentration of cAMP using a standard curve then dose response curves were plotted and inflection point (IP) values were determined.	B	10.17	pKi	0.07	nM	Ki	US-9833448-B2. Piperidinone carboxamide azaindane CGRP receptor antagonists (2017)
ChEMBL	NATIVE RECEPTOR BINDING ASSA: The binding of 125I-CGRP to receptors in SK-N-MC cell membranes was carried out essentially as described (Edvinsson et al. (2001) Eur. J. Pharmacol. 415, 39-44). Briefly, membranes (25 μg) were incubated in 1 mL of binding buffer [10 mM HEPES, pH 7.4, 5 mM MgCl2 and 0.2% bovine serum albumin (BSA)] containing 10 pM 125I-CGRP and antagonist. After incubation at room temperature for 3 h, the assay was terminated by filtration through GFB glass fibre filter plates (PerkinElmer) that had been blocked with 0.5% polyethyleneimine for 3 h. The filters were washed three times with ice-cold assay buffer (10 mM HEPES, pH 7.4 and 5 mM MgCl2), then the plates were air dried. Scintillation fluid (50 μL) was added and the radioactivity was counted on a Topcount (Packard Instrument). Data analysis was carried out by using Prism and the Ki was determined by using the Cheng-Prusoff equation (Cheng & Prusoff (1973) Biochem. Pharmacol. 22, 3099-3108).Cells expressing recombinant human CL receptor/RAMP1 were washed with PBS and harvested in harvest buffer containing 50 mM HEPES, 1 mM EDTA and Complete™ protease inhibitors (Roche). The cell suspension was disrupted with a laboratory homogenizer and centrifuged at 48,000 g to isolate membranes. The pellets were resuspended in harvest buffer plus 250 mM sucrose and stored at −70° C. For binding assays, 20 μg of membranes were incubated in 1 mL binding buffer (10 mM HEPES, pH 7.4, 5 mM MgCl2, and 0.2% BSA) for 3 h at room temperature containing 10 pM 125I-hCGRP (GE Healthcare) and antagonist. The assay was terminated by filtration through 96-well GFB glass fiber filter plates (PerkinElmer) that had been blocked with 0.05% polyethyleneimine. The filters were washed 3 times with ice-cold assay buffer (10 mM HEPES, pH 7.4, and 5 mM MgCl2). Scintillation fluid was added and the plates were counted on a Topcount (Packard). Non-specific binding was determined and the data analysis was carried out with the apparent dissociation constant (Ki) determined by using a non-linear least squares fitting the bound CPM data to the equation below:Y obsd = ( Y max - Y min ) ⁢ ( % ⁢ ⁢ I max - % ⁢ Imin ⁢ / ⁢ 100 ) + Y min + ( Y max - Y min ) ⁢ ( 100 - % ⁢ ⁢ I max ⁢ / ⁢ 100 ) 1 + ( [ Drug ] ⁢ / ⁢ K i ⁡ ( 1 + [ Radiolabel ] ⁢ / ⁢ K d ) nH Where Y is observed CPM bound, Ymax is total bound counts, Ymin is non specific bound counts, (Ymax−Ymin) is specific bound counts, % Imax is the maximum percent inhibition, % I min is the minimum percent inhibition, radiolabel is the probe, and the Kd is the apparent dissociation constant for the radioligand for the receptor as determined by hot saturation experiments.	B	10.17	pKi	0.07	nM	Ki	US-10272077-B2. Piperidinone carboxamide azaindane CGRP receptor antagonists (2019)
CGRP receptor in Human [GtoPdb: 48]

ChEMBL data shown on this page come from version 36:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]